An efficient synthesis, characterization and antibacterial activity of novel N'-arylidene-4-(2-(piperidin-1-yl) ethoxy) benzohydrazide derivatives Schiff bases
IOSR Journal of Applied Chemistry (IOSR-JAC) is a double blind peer reviewed International Journal that provides rapid publication (within a month) of articles in all areas of applied chemistry and its applications. The journal welcomes publications of high quality papers on theoretical developments and practical applications in Chemical Science. Original research papers, state-of-the-art reviews, and high quality technical notes are invited for publications.
Synthesis and antimicrobial activity of some methyl (4- (benzo[d]oxazol-2-yl)...QUESTJOURNAL
ABSTRACT: In the present study, a new series of methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate amine derived from methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate (4TO1-TO6) have been synthesized by reacting the thio methyl group with different amines in presence of ethenol. The structural assessment of the compounds (TO 1- TO 6) was made on the basis of spectral data. The synthesized compounds were screened for their in vitro growth inhibiting activity against different strains of bacteria and fungi viz., Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa, S. aureus, Candida albicans and Cryptococcus neoformans were compared with standard agents such as Norfloxacin (10μg/ml) and Amphotericin B (10μg/ml) using broth dilution method. Compounds exhibit moderate to high antibacterial and antifungal activity
Synthesis of substituted 1, 2, 4-triazole derivatives by Microwave irradiationIOSR Journals
Various substituted Triazole-Thiol containing different functional group have been synthesized by microwave method. The title product 1-[(3H-indol-2-ylamino) methyl]-4-phenyl-4, 5-dihydro-1H-1, 2, 4-triazole-3-thiol is synthesized by using amino benzothiazole. The final structures have been established on the basis of their chemical analysis and spectral data. All micro-wave synthesized compounds results into good yield as compared to conventional method of which fluoro substituted compound shows maximum yield.
Simple Synthesis of Some Novel Polyfunctionally Derivatives of 2H-Coumarin-2-...IOSRJAC
Compound (2) was prepared from the reaction of ethyl-2-oxo-2H-coumarin-3-carboxylate (1) with ethylcyanoacetate in ethanol containing a catalytic amount of piperidine as catalyst. Compound (2) is the key intermediate for the synthesis of several series of new compounds such as ((pyrimidine, tetrazine, piperidine, oxazepine)-2H-coumarin-2-one derivatives by reaction with selected reagents such as urea, cyanoacetamide, cyanoacetohydrazide, orthoaminophenol and 5-aminotriazole.
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Synthesis and antimicrobial activity of some methyl (4- (benzo[d]oxazol-2-yl)...QUESTJOURNAL
ABSTRACT: In the present study, a new series of methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate amine derived from methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate (4TO1-TO6) have been synthesized by reacting the thio methyl group with different amines in presence of ethenol. The structural assessment of the compounds (TO 1- TO 6) was made on the basis of spectral data. The synthesized compounds were screened for their in vitro growth inhibiting activity against different strains of bacteria and fungi viz., Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa, S. aureus, Candida albicans and Cryptococcus neoformans were compared with standard agents such as Norfloxacin (10μg/ml) and Amphotericin B (10μg/ml) using broth dilution method. Compounds exhibit moderate to high antibacterial and antifungal activity
Synthesis of substituted 1, 2, 4-triazole derivatives by Microwave irradiationIOSR Journals
Various substituted Triazole-Thiol containing different functional group have been synthesized by microwave method. The title product 1-[(3H-indol-2-ylamino) methyl]-4-phenyl-4, 5-dihydro-1H-1, 2, 4-triazole-3-thiol is synthesized by using amino benzothiazole. The final structures have been established on the basis of their chemical analysis and spectral data. All micro-wave synthesized compounds results into good yield as compared to conventional method of which fluoro substituted compound shows maximum yield.
Simple Synthesis of Some Novel Polyfunctionally Derivatives of 2H-Coumarin-2-...IOSRJAC
Compound (2) was prepared from the reaction of ethyl-2-oxo-2H-coumarin-3-carboxylate (1) with ethylcyanoacetate in ethanol containing a catalytic amount of piperidine as catalyst. Compound (2) is the key intermediate for the synthesis of several series of new compounds such as ((pyrimidine, tetrazine, piperidine, oxazepine)-2H-coumarin-2-one derivatives by reaction with selected reagents such as urea, cyanoacetamide, cyanoacetohydrazide, orthoaminophenol and 5-aminotriazole.
ER Publication,
IJETR, IJMCTR,
Journals,
International Journals,
High Impact Journals,
Monthly Journal,
Good quality Journals,
Research,
Research Papers,
Research Article,
Free Journals, Open access Journals,
erpublication.org,
Engineering Journal,
Science Journals,
Synthesis And Antibacterial Activity Of 3-[(3-Phenyl-5-Thioxo-1, 5-Dihydro-4h...inventionjournals
A series of 3-[(3-phenyl-5-thioxo-1,5-dihydro-4H-1,2,4-triazol-4-yl)imino]-1,3-dihydro-2Hindole-2-one derivatives were synthesised through the nucleophilic substitution at carbonyl carbon of Isatin. Structure of synthesized compounds were elucidated by using IR, 1H NMR & 13C NMR spectrometry. Synthesised compounds showed significant antibacterial activity against E.coli (ATCC 35218), S.aureus (ATCC 25323), E.faecalis (Clinical isolate), K. Pneumonia, P. aeruginosa (ATCC 27893) using agar well diffusion method.
A optimized process for the synthesis of a key starting material for etodolac...IOSR Journals
Abstract An optimized process developed for the synthesis of 7-ethyltryptophol, a key starting material for etodolac, a non steroidal anti- inflammatory drug. Starting from commercially available 2-ethylphenylhydrazine. HCl and dihydro furan with con. H2SO4 as a catalyst in N, N- dimethyl acetamide ( DMAc). H2O (1:1) as a solvent in 75% yield . the method is easy, inexpensive , without purification getting pure solid. The process is very clean, high yielding & high quality and operationally simple.
Keywords: Etodolac, 7-ethyl tryptophol, 2-ethyl phenyl hydrazine hydrochloride, N,N-dimethyl acetamide.
Role of mixed ligand Pd(II) and Pt(II)complexes in photooxygenation reactionIOSR Journals
Mixed ligand complexes of the formula [M (phen) bdt] where M= Pd (II) or Pt(II), phen =1,10-phenanthroline and bdt =1,2-benzenedithiolate have been synthesized and studied as photosensitizers of singlet molecular oxygen (1O2) production. It was observed that, Pt (II) complex shows a better photosensitizing ability as compared to its Pd (II) analogue. However, both Pd (II) and Pt (II) complexes act as chemical quenchers of 1O2, resulting in their photooxidation shown by decay of the respective complex. ThusPt (II) complex undergoes selfsensitizedphotooxidation by 1O2. The solvent dependence of this reaction is undertaken by performing the experiment using pure DMF(dimethyl formamide)and 10% H2O in DMF as solvent. The comparison of rate of decay of the Pt(II)and Pd(II) complexes show enhancement of the reaction in presence of water. The decay of the complex was monitored by recording the difference absorption spectra of the complex in the visible region after definite irradiation times. Involvement of 1O2 is further supported by quenching studies of this reaction using NaN3 as physical quencher of 1O2.
Synthesis, Characterization, Spectral (FT-IR, 1H, 13C NMR, Mass and UV) and B...Dr. Pradeep mitharwal
Bio-potent ligands, 2-hydroxy-N-phenylbenzamide hydrazinecarbothioamide(HPHTSCZH2) and 2-hydroxy-N-phenylbenzamide hydrazine carbodithioic benzyl ester (HPHCBESH2) have been synthesized by the condensation of 2-hydroxy-N-phenylbenzamide with hydrazinecarbothioamide and hydrazine carbodithioic benzyl ester, respectively and reacted with hydrated lanthanide chlorides. The coordination moieties of the ligands have been confirmed by various spectral studies. - See more at: http://www.sciencedomain.org/abstract.php?iid=271&id=16&aid=2488#sthash.6v3aFQIi.dpuf
A new Schiff base 4-chlorophenyl)methanimine
(6R,7R)-3-methyl-8-oxo-7-(2-phenylpropanamido)-5-thia-1-
azabicyclo[4.2.0]oct-2-ene-2-carboxylate= (HL)= C23H20
ClN3O4S) has been synthesized from β-lactam antibiotic
(cephalexin mono hydrate(CephH)=(C16H19N3O5S.H2O) and 4-
chlorobenzaldehyde . Figure(1) Metal mixed ligand complexes
of the Schiff base were prepared from chloride salt of
Fe(II),Co(II),Ni(II),Cu(II),Zn(II) and Cd (II), in 50% (v/v)
ethanol –water medium (SacH ) .in aqueous ethanol(1:1)
containing and Saccharin(C7H5NO3S) = sodium hydroxide.
Several physical tools in particular; IR, CHN, 1H NMR, 13C
NMR for ligand and melting point molar conductance, magnetic
moment. and determination the percentage of the metal in the
complexes by flame(AAS). The ligands and there metal
complexes were screened for their antimicrobial activity against
four bacteria (gram + ve) and (gram -ve) {Escherichia coli,
Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus}.
The proposed structure of the complexes using program, Chem
office 3D(2006). The general formula have been given for the
prepared mixed ligand complexes Na2[M(Sac)3(L)], M(II) = Fe
(II), Co(II) , Ni(II), Cu (II), Zn(II) , and Cd(II).
HL= C29H24 ClN3O4S, L= C29H23 ClN3O4S -.
A series of novel 5-[2-(4-fluorobenzyl)-6-aryl-imidazo[2,1-b][1,3,4]thiadiazol-5-ylmethylene] thiazolidine-2,4-dione derivatives (4a-d) were synthesized. These final compounds (4a-d) were synthesized by Knoevenagel condensation of 2-(4-fluorobenzyl)-6-arylimidazo[2,1-b][1,3,4]thiadiazole-5-carbaldehydes (3a-d) with thiazolidine-2,4-dione. All the newly synthesized compounds were screened for their invivo hypoglycemic and hypolipidemic activity in male Wister rats. The Structures of all the newly synthesized compounds were established by analytical and spectral data.
Design, Synthesis, Biological Evaluation, and In Silico ADMET Studies of 1,8-...BRNSS Publication Hub
In the present study, 1,8-naphthyridine-3-carboxylic acid derivatives (5a1, 5a2, 5b1, and 5b2) were
designed, synthesized, and screened for their in vitro H1-antihistaminic activity. H1R inhibitory activity
of the synthesized derivatives was calculated by the modified Van Arman technique, histamine-induced
bronchoconstriction in guinea pigs. A good bronchorelaxant effect of compounds was observed in
histamine-contracted guinea pig tracheal chain through H1-receptor antagonism. In addition, the
hypothetically resulted compounds are checked for their reliability on other in silico drug designing
online web services like SwissADME predictor. In silico ADMET analysis results show that all the
derivatives had negligible toxicity, good absorption, and solubility profile. These compounds may serve
as possible lead for establishing safe and effective antihistaminic agent(s).
SYNTHESIS OF OXAZIPEN COMPOUNDS VIA SCHIFF BASESJing Zang
This work involved preparation of cyclic compounds are containing of more than one hetero atoms in their structures like (N)-nitrogen atom. A seven-member ring compounds were prepared by condensation of N,N-di methyl amino benzaldehyde with aromatic amines to give compounds [N2-N17], these compounds were found to react with maleic anhydride to give 7-memberd ring [N18-N32]. All these compounds [N2- N32] were prepared by pericyclic reactions.
Synthesis, spectroscopic, magnetic properties and superoxide dismutase (SOD) ...IOSR Journals
Three new ternary copper(II) complexes formulated as [Cu(HIda)(bipy)] 1; [Cu(HIda)(phen)] 2; [Cu(HIda)(dmp)] 3; where HIda =N-(2-hydroxyethyl)-2- iminodiacetic acid ; bipy = 2, 2’- bipyridine; phen = 1,10- phenanthroline; dmp = 2,9-dimethyl 1,10-phenanthroline, have been synthesized and characterized by partial elemental analysis, FAB-mass (m/z), EPR, UV-visible and CV measurements. The magnetic and spectroscopic data of all these complexes 1-3 indicate distorted octahedral geometry. The EPR spectra of these complexes in frozen DMSO solutions showed a single at g ca. 2. The trend in g-value (g||>g>2.0023) suggests that the unpaired electron on copper (II) has dx2–y2 character. The SOD activities of the complexes have been investigated. Antibacterial and antifungal activity of these complexes were also measured and discussed.
Synthesis, characterization and biological activities of novel 2-mercaptobenz...ijperSS
ABSTRACT
A new series of Benzoxazol-2-ylthio-N-(4-substituted) acetohydrazide derivatives (IVa-IVk), were obtained by synthesising new Schiff’s bases derived from benzoxolyl-2-mercaptoaceto hydrazide derivatives by treating with various aryl/hetero aryl aldehydes. Their chemical structures have been confirmed by 1H-NMR, 13C-NMR, FT-IR and ESI-MS spectral data. The synthesised derivatives (IVa-IVk) were screened for their in vitro antimicrobial activities by agar diffusion method. Among the synthesized compounds IVb, IVe, and IVk shown strong antibacterial activity and the compounds IVb, IVe and IVf exhibited strong antifungal activity.
Key words: Benzoxazole, aryl/hetero aryl aldehydes, schiff’s bases, antibacterial activity, antifungal activity.
An Efficient Synthetic Approach Towards 4-Cyano-3-(Methylthio)-5-Oxo-2H-Pyraz...inventionjournals
ABSTRACT: Synthesis of novel heterocyclic 4-cyano -3-(methylthio)-5-oxo-2H-pyrazole-1(5H)- carbothioamide (3) was prepared by condensing ethyl-2-cyano-3,3-bis (methylthio)acrylate (1) with thiosemicarbazide (2) in DMF and catalytic amount of potassium carbonate. Compound (3) has methylthio group at third position, which is replaced by different nucleophiles such as substituted anilines| phenols| hetryl amines| compounds containing active methylene group to afford 3-substituted derivatives of compound (3). All the newly synthesized compounds were screened for their antimicrobial activity.
Synthesis And Antibacterial Activity Of 3-[(3-Phenyl-5-Thioxo-1, 5-Dihydro-4h...inventionjournals
A series of 3-[(3-phenyl-5-thioxo-1,5-dihydro-4H-1,2,4-triazol-4-yl)imino]-1,3-dihydro-2Hindole-2-one derivatives were synthesised through the nucleophilic substitution at carbonyl carbon of Isatin. Structure of synthesized compounds were elucidated by using IR, 1H NMR & 13C NMR spectrometry. Synthesised compounds showed significant antibacterial activity against E.coli (ATCC 35218), S.aureus (ATCC 25323), E.faecalis (Clinical isolate), K. Pneumonia, P. aeruginosa (ATCC 27893) using agar well diffusion method.
A optimized process for the synthesis of a key starting material for etodolac...IOSR Journals
Abstract An optimized process developed for the synthesis of 7-ethyltryptophol, a key starting material for etodolac, a non steroidal anti- inflammatory drug. Starting from commercially available 2-ethylphenylhydrazine. HCl and dihydro furan with con. H2SO4 as a catalyst in N, N- dimethyl acetamide ( DMAc). H2O (1:1) as a solvent in 75% yield . the method is easy, inexpensive , without purification getting pure solid. The process is very clean, high yielding & high quality and operationally simple.
Keywords: Etodolac, 7-ethyl tryptophol, 2-ethyl phenyl hydrazine hydrochloride, N,N-dimethyl acetamide.
Role of mixed ligand Pd(II) and Pt(II)complexes in photooxygenation reactionIOSR Journals
Mixed ligand complexes of the formula [M (phen) bdt] where M= Pd (II) or Pt(II), phen =1,10-phenanthroline and bdt =1,2-benzenedithiolate have been synthesized and studied as photosensitizers of singlet molecular oxygen (1O2) production. It was observed that, Pt (II) complex shows a better photosensitizing ability as compared to its Pd (II) analogue. However, both Pd (II) and Pt (II) complexes act as chemical quenchers of 1O2, resulting in their photooxidation shown by decay of the respective complex. ThusPt (II) complex undergoes selfsensitizedphotooxidation by 1O2. The solvent dependence of this reaction is undertaken by performing the experiment using pure DMF(dimethyl formamide)and 10% H2O in DMF as solvent. The comparison of rate of decay of the Pt(II)and Pd(II) complexes show enhancement of the reaction in presence of water. The decay of the complex was monitored by recording the difference absorption spectra of the complex in the visible region after definite irradiation times. Involvement of 1O2 is further supported by quenching studies of this reaction using NaN3 as physical quencher of 1O2.
Synthesis, Characterization, Spectral (FT-IR, 1H, 13C NMR, Mass and UV) and B...Dr. Pradeep mitharwal
Bio-potent ligands, 2-hydroxy-N-phenylbenzamide hydrazinecarbothioamide(HPHTSCZH2) and 2-hydroxy-N-phenylbenzamide hydrazine carbodithioic benzyl ester (HPHCBESH2) have been synthesized by the condensation of 2-hydroxy-N-phenylbenzamide with hydrazinecarbothioamide and hydrazine carbodithioic benzyl ester, respectively and reacted with hydrated lanthanide chlorides. The coordination moieties of the ligands have been confirmed by various spectral studies. - See more at: http://www.sciencedomain.org/abstract.php?iid=271&id=16&aid=2488#sthash.6v3aFQIi.dpuf
A new Schiff base 4-chlorophenyl)methanimine
(6R,7R)-3-methyl-8-oxo-7-(2-phenylpropanamido)-5-thia-1-
azabicyclo[4.2.0]oct-2-ene-2-carboxylate= (HL)= C23H20
ClN3O4S) has been synthesized from β-lactam antibiotic
(cephalexin mono hydrate(CephH)=(C16H19N3O5S.H2O) and 4-
chlorobenzaldehyde . Figure(1) Metal mixed ligand complexes
of the Schiff base were prepared from chloride salt of
Fe(II),Co(II),Ni(II),Cu(II),Zn(II) and Cd (II), in 50% (v/v)
ethanol –water medium (SacH ) .in aqueous ethanol(1:1)
containing and Saccharin(C7H5NO3S) = sodium hydroxide.
Several physical tools in particular; IR, CHN, 1H NMR, 13C
NMR for ligand and melting point molar conductance, magnetic
moment. and determination the percentage of the metal in the
complexes by flame(AAS). The ligands and there metal
complexes were screened for their antimicrobial activity against
four bacteria (gram + ve) and (gram -ve) {Escherichia coli,
Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus}.
The proposed structure of the complexes using program, Chem
office 3D(2006). The general formula have been given for the
prepared mixed ligand complexes Na2[M(Sac)3(L)], M(II) = Fe
(II), Co(II) , Ni(II), Cu (II), Zn(II) , and Cd(II).
HL= C29H24 ClN3O4S, L= C29H23 ClN3O4S -.
A series of novel 5-[2-(4-fluorobenzyl)-6-aryl-imidazo[2,1-b][1,3,4]thiadiazol-5-ylmethylene] thiazolidine-2,4-dione derivatives (4a-d) were synthesized. These final compounds (4a-d) were synthesized by Knoevenagel condensation of 2-(4-fluorobenzyl)-6-arylimidazo[2,1-b][1,3,4]thiadiazole-5-carbaldehydes (3a-d) with thiazolidine-2,4-dione. All the newly synthesized compounds were screened for their invivo hypoglycemic and hypolipidemic activity in male Wister rats. The Structures of all the newly synthesized compounds were established by analytical and spectral data.
Design, Synthesis, Biological Evaluation, and In Silico ADMET Studies of 1,8-...BRNSS Publication Hub
In the present study, 1,8-naphthyridine-3-carboxylic acid derivatives (5a1, 5a2, 5b1, and 5b2) were
designed, synthesized, and screened for their in vitro H1-antihistaminic activity. H1R inhibitory activity
of the synthesized derivatives was calculated by the modified Van Arman technique, histamine-induced
bronchoconstriction in guinea pigs. A good bronchorelaxant effect of compounds was observed in
histamine-contracted guinea pig tracheal chain through H1-receptor antagonism. In addition, the
hypothetically resulted compounds are checked for their reliability on other in silico drug designing
online web services like SwissADME predictor. In silico ADMET analysis results show that all the
derivatives had negligible toxicity, good absorption, and solubility profile. These compounds may serve
as possible lead for establishing safe and effective antihistaminic agent(s).
SYNTHESIS OF OXAZIPEN COMPOUNDS VIA SCHIFF BASESJing Zang
This work involved preparation of cyclic compounds are containing of more than one hetero atoms in their structures like (N)-nitrogen atom. A seven-member ring compounds were prepared by condensation of N,N-di methyl amino benzaldehyde with aromatic amines to give compounds [N2-N17], these compounds were found to react with maleic anhydride to give 7-memberd ring [N18-N32]. All these compounds [N2- N32] were prepared by pericyclic reactions.
Synthesis, spectroscopic, magnetic properties and superoxide dismutase (SOD) ...IOSR Journals
Three new ternary copper(II) complexes formulated as [Cu(HIda)(bipy)] 1; [Cu(HIda)(phen)] 2; [Cu(HIda)(dmp)] 3; where HIda =N-(2-hydroxyethyl)-2- iminodiacetic acid ; bipy = 2, 2’- bipyridine; phen = 1,10- phenanthroline; dmp = 2,9-dimethyl 1,10-phenanthroline, have been synthesized and characterized by partial elemental analysis, FAB-mass (m/z), EPR, UV-visible and CV measurements. The magnetic and spectroscopic data of all these complexes 1-3 indicate distorted octahedral geometry. The EPR spectra of these complexes in frozen DMSO solutions showed a single at g ca. 2. The trend in g-value (g||>g>2.0023) suggests that the unpaired electron on copper (II) has dx2–y2 character. The SOD activities of the complexes have been investigated. Antibacterial and antifungal activity of these complexes were also measured and discussed.
Synthesis, characterization and biological activities of novel 2-mercaptobenz...ijperSS
ABSTRACT
A new series of Benzoxazol-2-ylthio-N-(4-substituted) acetohydrazide derivatives (IVa-IVk), were obtained by synthesising new Schiff’s bases derived from benzoxolyl-2-mercaptoaceto hydrazide derivatives by treating with various aryl/hetero aryl aldehydes. Their chemical structures have been confirmed by 1H-NMR, 13C-NMR, FT-IR and ESI-MS spectral data. The synthesised derivatives (IVa-IVk) were screened for their in vitro antimicrobial activities by agar diffusion method. Among the synthesized compounds IVb, IVe, and IVk shown strong antibacterial activity and the compounds IVb, IVe and IVf exhibited strong antifungal activity.
Key words: Benzoxazole, aryl/hetero aryl aldehydes, schiff’s bases, antibacterial activity, antifungal activity.
Similar to An efficient synthesis, characterization and antibacterial activity of novel N'-arylidene-4-(2-(piperidin-1-yl) ethoxy) benzohydrazide derivatives Schiff bases
An Efficient Synthetic Approach Towards 4-Cyano-3-(Methylthio)-5-Oxo-2H-Pyraz...inventionjournals
ABSTRACT: Synthesis of novel heterocyclic 4-cyano -3-(methylthio)-5-oxo-2H-pyrazole-1(5H)- carbothioamide (3) was prepared by condensing ethyl-2-cyano-3,3-bis (methylthio)acrylate (1) with thiosemicarbazide (2) in DMF and catalytic amount of potassium carbonate. Compound (3) has methylthio group at third position, which is replaced by different nucleophiles such as substituted anilines| phenols| hetryl amines| compounds containing active methylene group to afford 3-substituted derivatives of compound (3). All the newly synthesized compounds were screened for their antimicrobial activity.
METALLO - BIOACTIVE COMPOUNDS AS POTENTIAL NOVEL ANTICANCER THERAPYijac123
Mono and bi-organometallic complexes of Cu(II), Ni(II), Mn(II), Zn(II) and Ag(I) complexes with
oxaloamide ligand has much potential as therapeutic and diagnostic agents. The ligand allows the
thermodynamic and kinetic reactivity of the metal ion to be controlled and also provide a scaffold for
functionalization. Specific examples involving the design of metal complexes as anticancer agents are
discussed. These complexes have been synthesized and characterized by (1H-NMR, mass, IR, UV-VIS,
ESR) spectra, magnetic moments and conductance measurements, elemental and thermal analyses. Molar
conductances in DMF solution indicates that, the complexes are non-electrolytes. The ESR spectra of solid
Cu(II) complexes (2-5) show an axial type indicating a d(X2-y2) ground state with a significant covalent
bond character. However, Mn(II) complex(9), shows an isotropic type indicating an octahedral geometry.
Cytotoxic evolution IC50 of the ligand and its complexes have been carried out. Cu(II) Complexes show
enhanced activity in comparison to the parent ligand or standard drug. Copper is enriched in various
human cancer tissues and is a co-factor essential for tumor angiogenesis processes. However, the use of
copper binding ligand to target tumor, copper could provide a novel strategy for cancer selective
treatment.
Synthesis, Characterization and Study of Antioxidant Activities of Some New P...IJRES Journal
A series of substituted pyrazoline derivatives 5(a-c) have been synthesized by the reaction of substituted chalcones 4(a-c) with isatinhydrazide. The starting materials, chalcones were prepared by clasien schimidt condensation of appropriate 1-hydroxy-2-acetonaphthone with substituted aldehydes in the presence of sodium hydroxide and in poly ethylene glycol (PEG-400). The structures of the synthesized compounds were confirmed by IR, 1HNMR & Mass spectral data. The synthesized compounds were screened for Antioxidant Activity by DPPH method.
Synthesis, Characterization and Biological Evaluation of Substitutedthiazolid...paperpublications3
Abstract: A new series of substituted thiazolidin-4-ones were synthesized and evaluated for anticancer activity by means of MTT assay method for improved anticancer activity .The structures of these synthesized compounds were established by means of IR,H NMR analysis.All the compounds were evaluated for their anticancer activity .Compounds TH10 & TH19 were found most active due to presence of electron withdrawing groups at appropriate position.
Synthesis and Crystal Structure of Anickel (II) and Zinc (II) Complex From 1,...IOSRJAC
:The title mononuclear nickel and zinc complexes, Ni(C11H9N4S3)2andZn(C11H9N4S3)2 .2(C3H7NO), were prepared by the reaction of Nickel(II) or Zinc(II)acetate with 1,5-bis[(2- thiophenyl)methylidene]thiocarbonohydrazide in a methanol solution. It features mono-deprotonated bisbidentate ligands, which coordinate to metal (II) ions by hydrazylN and thiocarbony lS atoms, yielding a tetracoordinated metal ions complexes. In Ni(II) complex the geometry around the metal ion is described as square planar. In the Zn(II) the metal atom shows severely tetrahedral distortion from anideal square-planar coordination geometry, as reflected by the dihedral angle between ZnN2and ZnS2 planes of 73.03(13)°. Two intramolecular hydrogen bonds are observed between the solvate dmf molecules and the coordinated ligands:N2—H2N…O1i and N6—H6N…O2 ii in this complex
Synthesis, Spectroscopic study & Biological Activity Of Some Organotin(Iv) De...IOSR Journals
Some di-and triorganotin(IV) derivatives of (2E)-N-methyl-(2
oxo1,2diphenylethylidne)hydrazinecarbothioamide synthesised by the reactions of the corresponding di and
triorganotin(IV) chlorides with the sodium salt of (2E)-N-methyl-(2-
oxo1,2diphenylethylidne)hydrazinecarbothioamide in different molar ratios. These derivatives have been
characterized by elemental analyses ,molecular weights, conductivity measurements and spectral(IR, 1H, 13C
and 119 Sn NMR) studies.
Mixed Ligand, Palladium(II) and Platinum(II) Complexes of Tertiary Diphosphin...Karwan Omer
Palladium(II) and platinum(II) complexes containing the mixed ligands tertiary
diphosphinesdppm. dppp and dppf with Thioester ligand S-1H benzo[d] imidazole-2-yl benzothioate
(HSBIBT) have been prepared by the reaction of PdCl2 and PtCl2 with one equiv of tertiary
diphosphines ligands to form [Pd(k2-dppf)Cl2], [Pd(k2-dppp)Cl2] and [Pt(k2-dppmCl)Cl2] complexes
and then add the ligand HSBIBT to these complexes to form mixed ligand complexes. The prepared
complexes have been characterized by single-crystal X-ray diffraction, elemental analysis, magnetic
susceptibility, molar conductance, IR spectral data and UV-Visible. The results suggested that the
ligand HSBIBT bonded to the metal through N atom and square planner geometries were assigned
for the complexes.
Synthesis, spectroscopic, electrochemical, magnetic properties and super oxid...IOSR Journals
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Cell utilize energy in the form of ATP.
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An efficient synthesis, characterization and antibacterial activity of novel N'-arylidene-4-(2-(piperidin-1-yl) ethoxy) benzohydrazide derivatives Schiff bases
1. IOSR Journal of Applied Chemistry (IOSR-JAC)
e-ISSN: 2278-5736.Volume 8, Issue 12 Ver. II (Dec. 2015), PP 06-11
www.iosrjournals.org
DOI: 10.9790/5736-081220611 www.iosrjournals.org 6 |Page
An efficient synthesis, characterization and antibacterial activity
of novel N'-arylidene-4-(2-(piperidin-1-yl) ethoxy)
benzohydrazide derivatives Schiff bases
Premlata Gupta, Kamal Jat, Vijendra Singh, Ruchi Shrivastava
(Department of chemistry IPS Academy, Indore, Madhya Pradesh, INDIA)
Abstract: A series of novel N'-arylidene-4-(2-(piperidin-1-yl)ethoxy)benzohydrazide derivatives (3a-3j) have
been synthesized from condensation reaction between 4-(2-(Piperidin-1-yl)ethoxy)benzohydrazide 2 and various
aldehyde. The structures of all these newly synthesized compounds were established on the basis of spectral
studies (IR, NMR & MASS) and Element analysis. The anti-microbial activities of these compounds were tested
in vitro by agar diffusion cup-plate method against two Gram-negative Escherichia coli, Pseudomonas
aeruginosa and two Gram-positive Staphylococcus aureus, Bacillus substilis bacteria and fungi Candida
albicans at 100 µg/ml concentration. All these compounds have displayed good or moderate activities against
the test microorganisms and all these inactive against C. albicans.
Keywords: Antimicrobial activity, hydrazones, piperdine derivatives, Schiff bases.
I. Introduction
Schiff bases are the most significant class of compounds that has gained much importance in recent
years due to their wide range of biological activities and industrial application. Compounds containing the
>C=N- (azomethine group) structure are known as Schiff bases, usually synthesized from the condensation of
primary amines with active carbonyl groups and they were first reported by Schiff in 1864[1]. These compounds
are also known as anils, imines or azomethines. These are found to posses many pharmacological activities such
as antimalarial[2], anticancer[3], antibacterial[4], antifungal[5], antitubercular[6], anti-inflammatory[7],
antioxidant[8], antiviral[9], anticonvulsant[10], antitumor[11], anti-HIV[12], cytotoxic[13], antidiabetic[14],
antihypertensive[15] and analgesic[16] etc. Besides some used as antifertility and enzymatic agents. Several
studies showed that the presence of a lone pair of electrons in sp2 hybridized orbital of nitrogen atom of the
azomethine group is played an important role in chemical and biological activity. Schiff bases are generally
excellent chelating agents[17] especially when a functional group like-OH or –SH is present close to the
azomethine group so as to form a five or six member ring with the metal ion. Versatility of Schiff base ligands
and biological, analytical and industrial applications of their complexes make further investigations in this area
highly desirable.
Based on the higher bio-reactivity of Schiff bases, we have decided to synthesize novel hydrazones
Schiff bases containing the piperidine moiety. All the synthesized compounds were characterized by IR, 1
H-
NMR, Mass spectral, elemental analysis and were screened for their anti-bacterial and anti-fungal activities. The
minimum inhibitory concentrations of the compounds were also measured by agar diffusion cup plate method.
II. Experiment
All chemicals and solvents were used of AR-grade. The melting points of all the synthesized
compounds were determined in one end open capillary tubes on a Buchi melting point apparatus. IR spectra
were recorded on Bruker FT-IR Spectrometer using KBr pellets in the range 4000-600 cm-1
. Proton nuclear
magnetic resonance (1H-NMR) spectra were recorded on Bruker 400 NMR spectrometer. Chemical shifts are
reported in parts per million (ppm) using tetraethyl silane (TMS) as an internal standard. Mass spectra recorded
a Waters mass spectrometer. IR, 1H-NMR and MS were consistent with assigned structure. Element analysis
(CHN) was undertaken with Thermo Scientific analyzer. The completion of reaction and purity of compounds
were checked on thin layer chromatography (TLC) on silica gel-G (Merck) coated aluminum plates, visualized
by ultra violet light 254 nm and developing solvents were chloroform-methanol (9:1).
2.1 Procedure for the preparation of methyl 4-(2-(piperidin-1-yl)ethoxy)benzoate(1)
Methyl 4-(2-(piperidin-1-yl)ethoxy)benzoate was prepared as reported in the literature (Das et al. 2013)
2.2 Procedure for the preparation of 4-(2-(piperidin-1-yl)ethoxy)benzohydrazide (2)
To a dry RBF 15.8g (0.06 mole) methyl 4-(2-(piperidin-1-yl)ethoxy)benzoate (1) and 60 ml hydrazine
hydrate were heated for 5 hrs at 90-100O
C. After completion of reaction (TLC), the reaction mixture cool to
2. An efficient synthesis, characterization and antibacterial activity of novel N'-arylidene-4-….
DOI: 10.9790/5736-081220611 www.iosrjournals.org 7 |Page
ambient temperature and poured in ice water, filtered, washed with water then recrystallized from absolute
ethanol. Product were dried in an oven at 60-65 0
C to give 13.50g 4-(2-(piperidin-1-yl)ethoxy)benzohydrazide.
M.P. 98-1000
C, yield 85.44%.
RI(cm-1
, KBr):-3401.71-3256.14 (NH2, N-H stretching), 3038.46(Aromatic C-H stretching ), 2935.38,
2826.39,2788.72(C-H stretching), 1655.35(C=O stretching), 1604(C-C stretching), 1512(N-H bending),
1342.68(C-O stretching).
MNR(400MHz, DMSO-d6), δ 9.51 (s, 1H, -NH), 7.22-7.90(m, 4H, Ar), 4.47(s, 2H,-NH2), 4.21 (t, 2H, OCH2),
2.71(t, 2H, OCCH2), 2.42(t, 4H, Py), 1.61(m, 2H, Py), 1.49(m, 4H, Py).
MS: m/z- 264.15 (M+
).
2.3 General Procedure for the preparation of Schiff bases(hydrazones) 3a-3j:-
To a dry RBF 1g (0.0038 mole) of 4-(2-(piperidin-1-yl)ethoxy)benzohydrazide(2) was refluxed with
equal mole of substituted aldehydes in 10 ml absolute ethanol for 5-8 hrs. After completion of reaction (TLC),
the reaction mixture cool to ambient temperature and the solid obtained was collected by filtration and
recrystallisation in ethanol. Product were dried in an oven at 60-65 0
C to give N'-arylidene-4-(2-(piperidin-1-
yl)ethoxy)benzohydrazide (3a-3j)
2.3.1 N’-benzylidene-4-(2-(piperidin-1-yl)ethoxy)benzohydrazide (3a)
IR(cm-1
, KBr) :3435.48,3217.07(N-H Stretching),3032.43(Aromatic C-H stretching ), 2937.39,
2851.29, 2801.69 (C-H stretching), 1648.04 (C=O),1607(C-C stretching),1563.96 (C=N stretching), 1508.13
(N-H bending), 1368.62 (C-O stretching), 1308.16 (C-N stretching).
1
H-NMR (400MHz, DMSO-d6), δ 11.70 (s, 1H, -NH), 8.46(s, 1H,N=CH), 7.0-8.18(d, 9H, Ar), 4.1(t, 2H, O-
CH2), 2.70(t, 2H, OCCH2), 2.52(t, 4H, Py), 1.52(m, 4H, Py), 1.41(t, 2H, Py).
MS: m/z- 352.16 (M+
).
2.3.2 N'-(4-chlorobenzylidene)-4-(2-(piperidin-1-yl)ethoxy)benzohydrazide (3b)
IR(KBr): 3431.27,3221.37(N-H Stretching),3042.71(Aromatic C-H stretching ), 2934.79, 2861.48,
2810.62 (C-H stretching), 1642.54 (C=O),1612.38(C-C stretching), 1567.40 (C=N stretching), 1511.49 (N-H
bending), 1360.73 (C-O stretching), 1301.00 (C-N stretching),715.16(C-Cl stretching),
1
H-NMR(400MHz, DMSO-d6) 11.71 (s, 1H, -NH), 8.45(s, 1H,N=CH), 7.20-8.25(d, 8H, Ar), 4.09(t, 2H, O-
CH2), 2.75(t, 2H, OCCH2), 2.51(t, 4H, Py), 1.54(m, 4H, Py), 1.41(t, 2H, Py).
MS: m/z- 386.12 (M+
).
2.3.3 N'-(4-bromobenzylidene)-4-(2-(piperidin-1-yl)ethoxy)benzohydrazide (3c)
IR(KBr): 3248.37(N-H Stretching),3052.71(Aromatic C-H stretching ), 2951.29, 2846.24, (C-H
stretching), 1649.54 (C=O),1614.34(C-C stretching), 1564.41 (C=N stretching), 1515.41 (N-H bending),
1364.41 (C-O stretching), 1308.42 (C-N stretching), 647.25(C-Br stretching).
1
H-NMR(400MHz, DMSO-d6) 11.74 (s, 1H, -NH), 8.42(s, 1H,N=CH), 7.35-8.34(d, 8H, Ar), 4.11(t, 2H, O-
CH2), 2.71(t, 2H, OCCH2),2.54(t, 4H, Py),1.59(m, 4H, Py),1.44(t, 2H, Py)
MS: m/z- 430.16 (M+
)
2.3.4 N'-(4-methylbenzylidene)-4-(2-(piperidin-1-yl)ethoxy)benzohydrazide (3d)
IR(KBr): 3238.57(N-H Stretching), 3038.32(Aromatic C-H stretching ), 2947.31, 2821.54, 2810.60 (C-
H stretching), 1651.44 (C=O),1609.23(C-C stretching),1557.76 (C=N stretching), 1528.14 (N-H bending),
1360.52 (C-O stretching), 1321.26 (C-N stretching)
1
H-NMR(400MHz, DMSO-d6) ), δ 11.68 (s, 1H, -NH), 8.44(s, 1H,N=CH), 6.91-8.17(d, 8H, Ar), 4.14(t, 2H, O-
CH2), 2.71(t, 2H, OCCH2), 2.46(t, 4H, Py), 2.35(s, 3H, CH3), 1.54(m, 4H, Py), 1.43(t, 2H, Py).
MS: m/z- 366.19 (M+
)
2.3.5 N'-(4-methoxybenzylidene)-4-(2-(piperidin-1-yl)ethoxy)benzohydrazide (3e)
IR(KBr): 3227.17(N-H Stretching),3036.40(Aromatic C-H stretching ), 2931.24, 2848.27, 2811.64 (C-
H stretching), 1645.14 (C=O),1611(C-C stretching),1559.57 (C=N stretching), 1507.43 (N-H bending), 1361.45
(C-O stretching), 1304.11 (C-N stretching)
1
H-NMR(400MHz, DMSO-d6) ), δ 11.70 (s, 1H, -NH), 8.44(s, 1H,N=CH), 7.16-8.19(d, 8H, Ar), 4.13(t, 2H, O-
CH2), 3.78(s, 3H, OCH3) 2.74(t, 2H, OCCH2), 2.52(t, 4H, Py),1.52(m, 4H, Py),1.44(t, 2H, Py),
MS: m/z- 381.16 (M+
)
4. An efficient synthesis, characterization and antibacterial activity of novel N'-arylidene-4-….
DOI: 10.9790/5736-081220611 www.iosrjournals.org 9 |Page
Scheme: - Synthesis routes for piperidine derivatives Schiff bases (3a-3j).
CONHN
OCH2CH2 N
COOCH3
OCH2CH2 N
COOCH3
OH
+
N
CH2CH2Cl
HCl K2CO3
CONHNH2
OCH2CH2 N
NH2NH2H2O
(1)
(2)(3a-3h)
CHAr
ArCHO
Where Ar is substituted phenyl, furanyl and thiophenyl
The chemical structure of the synthesized Schiff base (3a-3j) were characterization by FT-IR, 1H-
NMR, MS and elements analysis. The FT-IR spectra of the Schiff bases (3a-3j) showed absorption band at
3200-3450 cm-1
due to N-H stretching vibration , band at 1640-1655 cm-1
due to C=O stretching vibration and
band at 1560-1570 cm-1
due to azomethine group C=N stretching vibration. The nuclear magnetic resonance
(1H-NMR) of Schiff bases (3a-3j) showed singlet at δ 8.40-8.48 indicating presence of azomethine (-N=CH-)
proton. The sharp singlet at δ 10.88-11.72 indicating presence of - CONH- proton. In the mass spectrum, Schiff
bases (3a-3j) showed a peak at m/z, which matches its molecular formula. Physicochemical data and elemental
analysis results of the compounds are listed in Table 1. The spectral data of all the compounds are given in
Section 2
Table: - (1) Characterization data of compound 3a-3j
Compounds Ar- Molecular
Formula Melting
Point
( 0
C )
Yield
(%)
Elemental Analysis
Calc. / (Found)
C
(%)
H
(%)
N
(%)
3a C21H25N3O2 136-138 82.70
71.77
(71.75)
7.17
(7.20)
11.96
(11.95)
3b Cl C21H24ClN3O2 179-181 85.10
65.36
(65.37)
6.27
(6.29)
10.89
(10.88)
3c Br C21H24BrN3O2 202-204 86.45
58.65
(58.61)
5.64
(5.62)
9.75
(9.76)
3d CH3 C22H27N3O2 186-188 84.35
72.30
(72.33)
7.45
(7.42)
11.50
(11.52)
5. An efficient synthesis, characterization and antibacterial activity of novel N'-arylidene-4-….
DOI: 10.9790/5736-081220611 www.iosrjournals.org 10 |Page
3e OCH3 C22H27N3O3 190-192 83.56
69.27
(69.26)
7.13
(7.15)
11.02
(11.05)
3f OH C21H25N3O3 186-188 78.24
68.64
(68.67)
6.86
(6.85)
11.44
(11.42)
3g NO2 C21H24N4O4 175-176 86.17
63.62
(63.60)
6.10
(6.12)
14.13
(14.11)
3h N C23H30N4O2 212-214 82.95
70.02
(70.00)
7.67
(7.66)
14.20
(14.22)
3i
S
C19H23N3O2S 165-168 83.31
63.84
(63.87)
6.49
(6.48)
11.75
(11.73)
3j
O
C19H23N3O3 172-174 85.95
66.84
(66.83)
6.79
(6.81)
12.31
(12.29)
3.2 Antimicrobial Activity
The anti-bacterial and antifungal activities of the newly synthesized compounds 3a-3j were evaluated
by cup-plate agar diffusion method [19] by measuring the zone of inhibition in mm. All these Novel synthesized
compound screened against Gram-negative Escherichia coli, Pseudomonas aeruginosa. And Gram-positive
Staphylococcus aureus, Bacillus substilis bacteria and fungi Candida albicans at 100 µg/ml concentration. The
solvent used for the preparation of compound solutions (DMF) did not show inhibition against the tested
organisms (negative control). Ciprofloxacin and Fluconazole were used as standard for comparisons
antibacterial and antifungal activity. The results of antimicrobial activity of all the newly synthesized
compounds were presented in Table 2. Most of the compounds were inactive against C. albicans and all
compounds are moderately active but compounds 3g, 3i and 3j are showed good antibacterial activity.
Table:- (2) Antimicrobial activity of newly synthesized compound 3a-3j
Compounds Zone of inhibition (in mm)
E. coli P. aeruginosa M. luteus B. subtilis C. albicans
3a 06 08 04 09 -
3b 09 10 07 10 -
3c 08 10 06 08 -
3d 07 08 10 08 -
3e 10 11 09 09 -
3f 15 12 14 17 -
3g 17 19 13 16 -
3h 11 10 08 10 -
3i 22 19 19 21 -
3j 20 21 18 20 -
Ciprofloxacin 25 23 25 24 -
Fluconazole - - - - 26
IV. Conclusion
We have successfully developed a simple, effective and high yield synthetic procedure for the
synthesis of hydrazones Schiff bases (3a-3j). The structure of all these compounds have been confirmed by
spectroscopic (NMR, IR, MASS) and element analysis data. All the synthesized compounds were evaluated in
vitro for their antibacterial activities against two Gram-negative Escherichia coli, Pseudomonas aeruginosa and
two Gram-positive Staphylococcus aureus, Bacillus substilis bacteria and fungi Candida albicans at 100 µg/ml
concentration. It was observed that the compounds 3f, 3g, 3i, 3j showed good activity whereas rest of the
compound displayed moderate activity against bacterial strains and these compounds were found to be inactive
against Candida albicans.
Acknowledgement
We are thankful to SAIF Punjab University Chandigarh for providing CHN, NMR and MASS spectral
data and also thanks to Medilux Lab. Pvt. Ltd. for providing IR spectral data.
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