General Anaesthesia (Medicinal Chemistry)Yogesh Tiwari
General anaesthetics are group of drugs that produces loss of consciousness, and therefore, loss of all sensations.
The absolute loss of sensation is termed as anaesthesia.
General Anaesthesia (Medicinal Chemistry)Yogesh Tiwari
General anaesthetics are group of drugs that produces loss of consciousness, and therefore, loss of all sensations.
The absolute loss of sensation is termed as anaesthesia.
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Med chem lecture on Anticholinergic drugs for B.Pharm level in Nepal
Content from Foye's Principle of medicinal chemistry, my own thoughts and some articles
This ppt covers the classification, structures and IUPAC names, Mechanism of action and uses of individual drugs...under anticonvulsants topic..Side effects/metabolism are also given for few
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,...Dr. Ravi Sankar
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,TYPES,CAUSES OF HYPERTENSION, CLASSIFICATION, MECHANISM OF ACTION, SAR, ACE INHIBITORS, ARB , DIURETICS(WATER PILLS), TIPS TO STOP SILENT KILLER.
BY P. RAVISANKAR, VIGNAN PHARMACY COLLEGE, VADLAMUDI, GUNTUR,A.P, INDIA.
This ppt covers the classification of anti psychotics with structures and IUPAC names, MOA, uses, metabolism and side effects. Dopaminergic pathways also given
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Med chem lecture on Anticholinergic drugs for B.Pharm level in Nepal
Content from Foye's Principle of medicinal chemistry, my own thoughts and some articles
This ppt covers the classification, structures and IUPAC names, Mechanism of action and uses of individual drugs...under anticonvulsants topic..Side effects/metabolism are also given for few
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,...Dr. Ravi Sankar
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,TYPES,CAUSES OF HYPERTENSION, CLASSIFICATION, MECHANISM OF ACTION, SAR, ACE INHIBITORS, ARB , DIURETICS(WATER PILLS), TIPS TO STOP SILENT KILLER.
BY P. RAVISANKAR, VIGNAN PHARMACY COLLEGE, VADLAMUDI, GUNTUR,A.P, INDIA.
This ppt covers the classification of anti psychotics with structures and IUPAC names, MOA, uses, metabolism and side effects. Dopaminergic pathways also given
Heterocyclic chemistry - Fused ring systemsNaresh Babu
Fused hetero cyclic ring systems like Quinoline, Isoquinoline, Indole, Acridine, Benzimidzole & Phenothiazine - Structure, Aromaticity, Preparations, Acidity-Basicity and characteristic chemical reactions
I hope You all like it. I hope It is very beneficial for you all. I really thought that you all get enough knowledge from this presentation. This presentation is about materials and their classifications. After you read this presentation you knowledge is not as before.
it's our aim to provide notes for pharmacy student without any charge.so that we make pharmacy education easier.
किसी भी शुल्क के बिना फार्मेसी छात्र के लिए नोट्स प्रदान करना हमारा लक्ष्य है।ताकि हम फार्मेसी शिक्षा को आसान बना दें।
I hope You all like it. I hope It is very beneficial for you all. I really thought that you all get enough knowledge from this presentation. This presentation is about materials and their classifications. After you read this presentation you knowledge is not as before.
The Art Pastor's Guide to Sabbath | Steve ThomasonSteve Thomason
What is the purpose of the Sabbath Law in the Torah. It is interesting to compare how the context of the law shifts from Exodus to Deuteronomy. Who gets to rest, and why?
This is a presentation by Dada Robert in a Your Skill Boost masterclass organised by the Excellence Foundation for South Sudan (EFSS) on Saturday, the 25th and Sunday, the 26th of May 2024.
He discussed the concept of quality improvement, emphasizing its applicability to various aspects of life, including personal, project, and program improvements. He defined quality as doing the right thing at the right time in the right way to achieve the best possible results and discussed the concept of the "gap" between what we know and what we do, and how this gap represents the areas we need to improve. He explained the scientific approach to quality improvement, which involves systematic performance analysis, testing and learning, and implementing change ideas. He also highlighted the importance of client focus and a team approach to quality improvement.
Unit 8 - Information and Communication Technology (Paper I).pdfThiyagu K
This slides describes the basic concepts of ICT, basics of Email, Emerging Technology and Digital Initiatives in Education. This presentations aligns with the UGC Paper I syllabus.
Operation “Blue Star” is the only event in the history of Independent India where the state went into war with its own people. Even after about 40 years it is not clear if it was culmination of states anger over people of the region, a political game of power or start of dictatorial chapter in the democratic setup.
The people of Punjab felt alienated from main stream due to denial of their just demands during a long democratic struggle since independence. As it happen all over the word, it led to militant struggle with great loss of lives of military, police and civilian personnel. Killing of Indira Gandhi and massacre of innocent Sikhs in Delhi and other India cities was also associated with this movement.
Synthetic Fiber Construction in lab .pptxPavel ( NSTU)
Synthetic fiber production is a fascinating and complex field that blends chemistry, engineering, and environmental science. By understanding these aspects, students can gain a comprehensive view of synthetic fiber production, its impact on society and the environment, and the potential for future innovations. Synthetic fibers play a crucial role in modern society, impacting various aspects of daily life, industry, and the environment. ynthetic fibers are integral to modern life, offering a range of benefits from cost-effectiveness and versatility to innovative applications and performance characteristics. While they pose environmental challenges, ongoing research and development aim to create more sustainable and eco-friendly alternatives. Understanding the importance of synthetic fibers helps in appreciating their role in the economy, industry, and daily life, while also emphasizing the need for sustainable practices and innovation.
1. Benzodiazepines
All benzodiazepines have a
benzene ring attached to a
diazepine ring.
In the green circles are
benzene rings and in the red
circle is a diazepine ring, with
the whole 1,4-benzodiazepine
system being in the blue ring
(the 1 and 4 denote the
position of the nitrogen atoms
in the ring
2. Benzodiazepines
Different benzodiazepines have been developed through chemical
substitutions at two major positions on the benzodiazepine
structure
Therefore, all benzodiazpines are simply variations on the same
core chemical structure.
3. Benzodiazepine
R1 R2 R3 R4
a CH3 H H Cl
b CH3 H F Cl
c H H H NO2
d H H Cl NO2
a. diazepam b.flutoprazepam c. nitrazepam
d. clonazepam
4. Modification: (triazole or imidazole)
estazolam, alprazolam, trizolam and
midazolam
N
N
(Z)
Cl
N
R2
R1 N
N
N
(E)
Cl
F
H3C N
R1 R2
estazolam H H
alprazolam CH3 H
trizolam CH3 Cl
Midazolam CH3 F
5. The duration of action for an individual
benzodiazepine depends on two factors:
1- the half-life and
2- the metabolic fate
9. Structure- activity relationship:
• The electron attractive substituents on ring A
enforce the activity
NO2>Br>CF3>Cl
• Ring B is necessary for activity
• The electron attractive substituents with small
volume on benzene ring of C-5 will enforce the
activity
• The hydrolysis of amide and imine
10. Ring A
•The minimum requirement for 5-phenyl
1,4 benzodiaipin 2one derivatives to
BZR include an aromatic or
hetroaromatic ring
•It is believed to participate in pi-pi
bonding with aromatic residue of
aromatic amino acids of the receptor
•The substitution on this ring produces
varied effect on binding with the
receptor, however such effects are not
predictable on the basis of electronic and
stearic properties
11. •An electronegative group (halo or
nitro) substituted at 7-position
markedly increase activity and
binding affinity
•Substitution on 6,8 and 9 decrease
the activity
•On the other hand 1-4 diazepine
derivative having ring A replaced
with hetrocyclic ring have weak
activity and affinity as compared to
phenyl derivatives
12. Ring B
A proton accepting group (carbonyl oxygen) at 2-
position of ring B is necessary to interact with
receptor histidine residue that act as proton donor and
help in ligand binding
Electron donating group must be in the same plane
with electronegative group on ring A, favoring a
coplanar spatial orientation of two moieties
Substitution of O with S effect selective binding
GABA BZR sub-populations but anxiolytic activity is
maintained
Substitution 3-position methylene or imine nitrogen is
sterically unfavorable
Derivatives having 3-hydroxy moiety have
comparable potency to non-hydroxylated analogue
but are excreted faster
13. Esterification of 3-hydroxy moiety is
possible without loss of activity
1-poition amide nitrogen and its
substituent are not required for in vitro
binding with BZR because many N-alkyl
side chains don’t decrease BZR affinity
Neither 4,5 double bond nor the nitrogen
of 4-position is required for activity
If C=N is reduced BZR affinity is
decreased but the derivatives again
oxidized in the body to C=N
14. Ring C
The 5-phenyl ring C is not required for
binding to the BZR in vitro, however, this
aromatic ring contribute favorable hydrphobic
or steric interactions to receptor binding and
its relationship to ring A
Substitution at 4' (para position) is
unfavorable for activity, however, ortho
substitution is not detrimental to agonist
activity
15. Annelating the 1,2 bond of ring B with an
additional electron rich ring such as triazole
(alprazolam) or imidazole (midazolam)
results in pharmacologically active
benzodiazepine derivatives with high
affinity to BZR
triazole
imidazole