Dear students, you can watch the Complete chapter of antibiotics in these videos as per PCI syllabus
1)Antibiotics-History & Introduction
https://www.youtube.com/watch?v=xdKch...
2)Easy Learning Of Chapter - β-Lactam antibiotics-Cephalosporin
https://www.youtube.com/watch?v=D7b5g...
3)Learn Complete Topic -β-Lactam antibiotics(Penicillin) in Medicinal Chemistry
https://www.youtube.com/watch?v=qXQ3S...
Dear students, you can watch the Complete chapter of antibiotics in these videos as per PCI syllabus
1)Antibiotics-History & Introduction
https://www.youtube.com/watch?v=xdKch...
2)Easy Learning Of Chapter - β-Lactam antibiotics-Cephalosporin
https://www.youtube.com/watch?v=D7b5g...
3)Learn Complete Topic -β-Lactam antibiotics(Penicillin) in Medicinal Chemistry
https://www.youtube.com/watch?v=qXQ3S...
Aminoglycosides(medicinal chemistry by p.ravisankar)Dr. Ravi Sankar
Aminoglycosides,Aminocyclitols,Source,Structures of streptomycin,Dihydrostreptomycin,A mention of other aminoglycoside antibiotics,Acid hydrolysis,Mechanism of action,SAR,Dihydrostreptomycin and its importance,therapeutic uses, toxicity.
penicillins - power point - History,mechanism of action,classification,chemis...Dr. Ravi Sankar
Antibiotics - Penicillin's - power point - History, mechanism of action, classification, chemistry, SAR, Nomenclature, uses, side effects- Medicinal chemistry.
Prof. P. Ravisankar M. Pharm., Ph.D.
HOD .,
Vignan Pharmacy college
vadlamudi- Guntur-A.P, India.
banuman35@gmail.com
Phone: 0 9059994000
0 9000199106
Definition
History
Chemistry
Properties
Classification & its Generation
Pharmacokinetics
Mechanism of action
Indication
Contraindication
Therapeutic use
Adverse effect
Resistance
Comparison with penicillin
Market preparation
These are antibiotics having a macrocyclic
lactone ring with attached sugars. Erythromycin
is the first member discovered in the 1950s,
Roxithromycin, Clarithromycin and Azithromycin
are the later additions. Antimicrobial spectrum is narrow,
includes mostly gram-positive and a few gramnegative
bacteria, and overlaps considerably with
that of penicillin G. Erythromycin is highly active
against Str. pyogenes and Str. pneumoniae, N.
gonorrhoeae, Clostridia, C. diphtheriae and
Listeria, but penicillin-resistant Staphylococci
and Streptococci are now resistant to erythromycin
also.
All cocci readily develop resistance
to erythromycin, mostly by acquiring the
capacity to pump it out. Resistant Enterobacteriaceae
have been found to produce an erythromycin
esterase. Alteration in the ribosomal binding
site for erythromycin by a plasmid encoded
methylase enzyme is an important mechanism of
resistance in gram-positive bacteria. All the above
types of resistance are plasmid mediated. Change
in the 50S ribosome by chromosomal mutation
reducing macrolide binding a
Macrolides are a class of antibiotics derived from Saccharopolyspora erythraea (originally called Streptomyces erythreus), a type of soil-borne bacteria.
-a broad-spectrum antibiotics.
-It is commonly used to treat acne, infection, and other infections caused by bacteria.
-The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
Aminoglycosides(medicinal chemistry by p.ravisankar)Dr. Ravi Sankar
Aminoglycosides,Aminocyclitols,Source,Structures of streptomycin,Dihydrostreptomycin,A mention of other aminoglycoside antibiotics,Acid hydrolysis,Mechanism of action,SAR,Dihydrostreptomycin and its importance,therapeutic uses, toxicity.
penicillins - power point - History,mechanism of action,classification,chemis...Dr. Ravi Sankar
Antibiotics - Penicillin's - power point - History, mechanism of action, classification, chemistry, SAR, Nomenclature, uses, side effects- Medicinal chemistry.
Prof. P. Ravisankar M. Pharm., Ph.D.
HOD .,
Vignan Pharmacy college
vadlamudi- Guntur-A.P, India.
banuman35@gmail.com
Phone: 0 9059994000
0 9000199106
Definition
History
Chemistry
Properties
Classification & its Generation
Pharmacokinetics
Mechanism of action
Indication
Contraindication
Therapeutic use
Adverse effect
Resistance
Comparison with penicillin
Market preparation
These are antibiotics having a macrocyclic
lactone ring with attached sugars. Erythromycin
is the first member discovered in the 1950s,
Roxithromycin, Clarithromycin and Azithromycin
are the later additions. Antimicrobial spectrum is narrow,
includes mostly gram-positive and a few gramnegative
bacteria, and overlaps considerably with
that of penicillin G. Erythromycin is highly active
against Str. pyogenes and Str. pneumoniae, N.
gonorrhoeae, Clostridia, C. diphtheriae and
Listeria, but penicillin-resistant Staphylococci
and Streptococci are now resistant to erythromycin
also.
All cocci readily develop resistance
to erythromycin, mostly by acquiring the
capacity to pump it out. Resistant Enterobacteriaceae
have been found to produce an erythromycin
esterase. Alteration in the ribosomal binding
site for erythromycin by a plasmid encoded
methylase enzyme is an important mechanism of
resistance in gram-positive bacteria. All the above
types of resistance are plasmid mediated. Change
in the 50S ribosome by chromosomal mutation
reducing macrolide binding a
Macrolides are a class of antibiotics derived from Saccharopolyspora erythraea (originally called Streptomyces erythreus), a type of soil-borne bacteria.
-a broad-spectrum antibiotics.
-It is commonly used to treat acne, infection, and other infections caused by bacteria.
-The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
002. Cephalosporins for students 2023 Prof. P. Ravisankar.pdfDr. Ravi Sankar
Cephalosporins, Why Cephalosporins? Advantages of cephalosporins over penicillin, Mechanism of action of cephalosporins, Classification of cephalosporins, Structures of some important cephalosporins and cephamycins, Oximinocephalosporins, SAR of cephalosporins,Hydrolytic reactions, degradation and stability of cephalosporins, Uses of cephalosporins, Comparison between 6-APA and 7-ACA and penam and cepham.
1a. Prof. P. Ravisankar, Vignan Pharmacy College, Vadlamudi, Guntur, AP., Ind...Dr. Ravi Sankar
Antibiotics, characteristics of an antibiotic, Brief historical background of antibiotics, Modern History of antibiotics, Classification of antibiotics, four groups of beta-lactam antibiotics, Classification of Penicillins, Penicillinase resistant Penicillins, Narrow spectrum anti-staphylococcal Penicillins, Amino Penicillins, Nomenclature of Penicillins, Stereochemistry of Penicillins, Hydrolysis of Penicillins, SAR of Penicillins, Mechanism of Penicillins, Beta-lactamase inhibitors, Therapeutic uses of Penicillins, Penicillin advantages, and disadvantages, Hypersensitivity or allergic reactions of Penicillins.
Tetracyclines are Octahydro napthacene derivatives which are bacteriostatic potent broad spectrum antibiotics and are the most widely prescribed form of antibiotic after penicillins.
TETRA means = four
CYCL means = hydrocarbon rings
INE means = derivation.
Tetracyclines are introduced 50 years ago as potent broad spectrum antibiotics.
They are biosynthesized form acetic acid and propionic acid units in microorganisms.
Finally, one of the best ways of reducing cancer is …..
Cancer prevention is an essential component of all cancer control plans because about 40 % of cancers are preventable.
Firstly…Public education campaigns are important in highlighting the dangers of smoking because possibly as many as 22 % (in the UK 30%) of cancers are caused by smoking.
Secondly, another 30% of cancers are diet-related. Decades of research have clearly shown that by living a healthy life, people can reduce the risk of developing the disease.
Screening tests help in finding Cancer earlier before developing any symptoms.
The benefits of eating high-fiber foods, fruit, and vegetables.
Epigallocatechin gallate, an antioxidant present in green tea, is another potential protective agent.
Finally, The new research funded by the UK and USA which aims to show the number of cancer cases could be prevented by known lifestyle and environmental factors,
like being a non-smoker, keeping a healthy weight, drinking less alcohol, eating a healthy balanced diet, and avoiding being exposed to certain infections or radiation.
Every country, regardless of resource level, can take steps to curb the cancer epidemic, save lives and prevent unnecessary suffering.
Finally, cancer prevention efforts should be preceded by a systematic planning process on cancer control.
Antibiotics definition, Early and modern history, classification of antibiotics, Mechanism of antibacterial action, bacterial cell and drug targets, penicillins nomenclature, degradation reactions of penicillins, medical classification of penicillins, SAR of penicillins, Mechanism of penicillins, Betalactamase inhibitors, Therapeutic uses of penicillins, toxicity of penicillins, Side effects of penicillins.
NOVEL SEPARATION AND QUANTITATIVE DETERMINATION OF LEVOFLOXACIN, PRULIFLOXACI...Dr. Ravi Sankar
The core AIM of the present study is to develop a novel, rapid, precise and accurate RP-HPLC method for simultaneous separation and quantification of six fluoroquinolones OF LEVOFLOXACIN (LEVO), PRULIFLOXACIN (PRFX), GATIFLOXACIN (GATI), SPARFLOXACIN (SPAR), MOXIFLOXAXIN (MOXI) AND BALOFLOXACIN (BALO) for the the day to day analysis.
The author felt that a novel single method for separation and quantification of all the above said drugs on single chromatographic system without any minor changes in detection wavelength and mobile phase composition.
To develop rapid, sensitive and economical analytical method based on HPLC for separation and estimation of six fluoroquinolones pharmaceutical dosage forms.
To develop method with shorter run time and better sensitivity.
Reducing the solvent consumption to make it more eco-friendly.
Avoid the column damage by minimizing the buffer strength and pH of mobile phase than reported methods.
To validate the method for different parameters like Accuracy, Precision, Linearity, specificity, Robustness International Conference on Harmonization ICH Q2(R1) guidelines..
To apply the developed RP-HPLC method in the analysis of pharmaceutical formulations.
Analytical method development and validation of novel Levofloxacin, Pruliflox...Dr. Ravi Sankar
For the first time simple, selective, sensitive RP-HPLC method was developed for the separation and quantitative development of LEVO, PRFX, GATI, SPAR, MOXI and BALO relating to fluoroquinolone anti bacterials in pharmaceutical dosage forms. The most important advantage of developed method was that the 6 separate drugs can be determined on a single chromatographic system without modifications in detection wavelength and mobile phase by RP-HPLC. The chromatographic separation of the selected drugs was carried out on Welchrom C18 column consisting of 250 mm X 4.6 mm, 5 µm particle size utilizing mixture of 10 mM phosphate buffer (pH 3.1): Acetonitrile in the ratio of 70:30,v/v as mobile phase at the flow rate of 1mL/min with detection wave length at 293 nm by using UV spectrophotometric detector with total run time of 10 minutes and 3.613, 4.230, 4.707, 5.497, 5.880 and 6.253 minutes of retention time obtained for LEVO, PRFX, GATI, SPAR, MOXI and BALO respectively. All calibration curves for six drugs showed indicated linearity over a concentration range of 2-10 µg/mL. The results regarding to limit of detection (LOD) and limit of quantitation (LOQ) for LEVO, PRFX, GATI, SPAR, MOXI and BALO were found to be 0.116 µg/mL and 0.348 µg/mL; 0.152 µg/mL and 0.460 µg/mL; 0.084 µg/mL and 0.255 µg/mL; 0.186 µg/mL and 0.558 µg/mL, 0.162 and 0.493, 0.112 and 0.390 respectively. These results clearly show low values of LOD and LOQ. The said developed method was ultimately utilized for quantification of marketed formulation.
NOVEL SIMULTANEOUS SEPARATION AND QUANTITATIVE DETERMINATION OF FOUR SARTANS...Dr. Ravi Sankar
The core AIM of the present study is to develop a novel, rapid, precise and accurate RP-HPLC method for simultaneous separation and quantification of Hydrochlorothiazide along with four sartans Telmisartan(TELM), Losartan(LOSA), Olmesartan(OLME) and Valsartan(VALS).
To develop Novel methods for separation and quantification of all the above said drugs on single chromatographic system without any minor changes in detection wavelength and mobile phase composition.
Total quality management (TQM), and current Good Manufacturing Practice (cGMP...Dr. Ravi Sankar
TQM, cGMP, Introduction, Definition, Importance, TQM frame work, Key concepts (Principles) of TQM, specific steps in the cycle, Benefits of TQM, cGMP, principles of GMP, Improtance of GMP, why GMP established?, difference between GMP and cGMP, GMP and cGMP regulations, code of federal regulations.
Tetracyclines BY Dr. P. Ravisankar M. Pharm., Ph.D.Dr. Ravi Sankar
Tetracyclines by Dr. P. Ravisankar M. Pharm., Ph.D.
Definition
Introduction
Classification
Historical background
Sources
Chemistry
SAR of tetracyclines
Mechanism of action of tetracyclines
Spectrum of activity
Uses of tetracyclines
Side effects of tetracyclines
Dr. P. Ravisankar M. Pharm., Ph.D.
Vitamin A
Vitamin D
Vitamin E
Vitamin K
Definition
Introduction
Classification
Structures,Functions,Deficiency,Diseases,Toxicity and uses.
Introduction to diuretics.
Therapeutic approaches.
Normal physiology of urine formation.
Classification of drugs .
Mechanism of action of Acetazolamide.
Mechanism of action of Thiazides.
Mechanism of action of Loop diuretics.
Mechanism of action of potassium sparing diuretics &aldosterone antagonists.
The Art of the Pitch: WordPress Relationships and SalesLaura Byrne
Clients don’t know what they don’t know. What web solutions are right for them? How does WordPress come into the picture? How do you make sure you understand scope and timeline? What do you do if sometime changes?
All these questions and more will be explored as we talk about matching clients’ needs with what your agency offers without pulling teeth or pulling your hair out. Practical tips, and strategies for successful relationship building that leads to closing the deal.
GDG Cloud Southlake #33: Boule & Rebala: Effective AppSec in SDLC using Deplo...James Anderson
Effective Application Security in Software Delivery lifecycle using Deployment Firewall and DBOM
The modern software delivery process (or the CI/CD process) includes many tools, distributed teams, open-source code, and cloud platforms. Constant focus on speed to release software to market, along with the traditional slow and manual security checks has caused gaps in continuous security as an important piece in the software supply chain. Today organizations feel more susceptible to external and internal cyber threats due to the vast attack surface in their applications supply chain and the lack of end-to-end governance and risk management.
The software team must secure its software delivery process to avoid vulnerability and security breaches. This needs to be achieved with existing tool chains and without extensive rework of the delivery processes. This talk will present strategies and techniques for providing visibility into the true risk of the existing vulnerabilities, preventing the introduction of security issues in the software, resolving vulnerabilities in production environments quickly, and capturing the deployment bill of materials (DBOM).
Speakers:
Bob Boule
Robert Boule is a technology enthusiast with PASSION for technology and making things work along with a knack for helping others understand how things work. He comes with around 20 years of solution engineering experience in application security, software continuous delivery, and SaaS platforms. He is known for his dynamic presentations in CI/CD and application security integrated in software delivery lifecycle.
Gopinath Rebala
Gopinath Rebala is the CTO of OpsMx, where he has overall responsibility for the machine learning and data processing architectures for Secure Software Delivery. Gopi also has a strong connection with our customers, leading design and architecture for strategic implementations. Gopi is a frequent speaker and well-known leader in continuous delivery and integrating security into software delivery.
Slack (or Teams) Automation for Bonterra Impact Management (fka Social Soluti...Jeffrey Haguewood
Sidekick Solutions uses Bonterra Impact Management (fka Social Solutions Apricot) and automation solutions to integrate data for business workflows.
We believe integration and automation are essential to user experience and the promise of efficient work through technology. Automation is the critical ingredient to realizing that full vision. We develop integration products and services for Bonterra Case Management software to support the deployment of automations for a variety of use cases.
This video focuses on the notifications, alerts, and approval requests using Slack for Bonterra Impact Management. The solutions covered in this webinar can also be deployed for Microsoft Teams.
Interested in deploying notification automations for Bonterra Impact Management? Contact us at sales@sidekicksolutionsllc.com to discuss next steps.
Search and Society: Reimagining Information Access for Radical FuturesBhaskar Mitra
The field of Information retrieval (IR) is currently undergoing a transformative shift, at least partly due to the emerging applications of generative AI to information access. In this talk, we will deliberate on the sociotechnical implications of generative AI for information access. We will argue that there is both a critical necessity and an exciting opportunity for the IR community to re-center our research agendas on societal needs while dismantling the artificial separation between the work on fairness, accountability, transparency, and ethics in IR and the rest of IR research. Instead of adopting a reactionary strategy of trying to mitigate potential social harms from emerging technologies, the community should aim to proactively set the research agenda for the kinds of systems we should build inspired by diverse explicitly stated sociotechnical imaginaries. The sociotechnical imaginaries that underpin the design and development of information access technologies needs to be explicitly articulated, and we need to develop theories of change in context of these diverse perspectives. Our guiding future imaginaries must be informed by other academic fields, such as democratic theory and critical theory, and should be co-developed with social science scholars, legal scholars, civil rights and social justice activists, and artists, among others.
Smart TV Buyer Insights Survey 2024 by 91mobiles.pdf91mobiles
91mobiles recently conducted a Smart TV Buyer Insights Survey in which we asked over 3,000 respondents about the TV they own, aspects they look at on a new TV, and their TV buying preferences.
Builder.ai Founder Sachin Dev Duggal's Strategic Approach to Create an Innova...Ramesh Iyer
In today's fast-changing business world, Companies that adapt and embrace new ideas often need help to keep up with the competition. However, fostering a culture of innovation takes much work. It takes vision, leadership and willingness to take risks in the right proportion. Sachin Dev Duggal, co-founder of Builder.ai, has perfected the art of this balance, creating a company culture where creativity and growth are nurtured at each stage.
Neuro-symbolic is not enough, we need neuro-*semantic*Frank van Harmelen
Neuro-symbolic (NeSy) AI is on the rise. However, simply machine learning on just any symbolic structure is not sufficient to really harvest the gains of NeSy. These will only be gained when the symbolic structures have an actual semantics. I give an operational definition of semantics as “predictable inference”.
All of this illustrated with link prediction over knowledge graphs, but the argument is general.
"Impact of front-end architecture on development cost", Viktor TurskyiFwdays
I have heard many times that architecture is not important for the front-end. Also, many times I have seen how developers implement features on the front-end just following the standard rules for a framework and think that this is enough to successfully launch the project, and then the project fails. How to prevent this and what approach to choose? I have launched dozens of complex projects and during the talk we will analyze which approaches have worked for me and which have not.
GraphRAG is All You need? LLM & Knowledge GraphGuy Korland
Guy Korland, CEO and Co-founder of FalkorDB, will review two articles on the integration of language models with knowledge graphs.
1. Unifying Large Language Models and Knowledge Graphs: A Roadmap.
https://arxiv.org/abs/2306.08302
2. Microsoft Research's GraphRAG paper and a review paper on various uses of knowledge graphs:
https://www.microsoft.com/en-us/research/blog/graphrag-unlocking-llm-discovery-on-narrative-private-data/
Dev Dives: Train smarter, not harder – active learning and UiPath LLMs for do...UiPathCommunity
💥 Speed, accuracy, and scaling – discover the superpowers of GenAI in action with UiPath Document Understanding and Communications Mining™:
See how to accelerate model training and optimize model performance with active learning
Learn about the latest enhancements to out-of-the-box document processing – with little to no training required
Get an exclusive demo of the new family of UiPath LLMs – GenAI models specialized for processing different types of documents and messages
This is a hands-on session specifically designed for automation developers and AI enthusiasts seeking to enhance their knowledge in leveraging the latest intelligent document processing capabilities offered by UiPath.
Speakers:
👨🏫 Andras Palfi, Senior Product Manager, UiPath
👩🏫 Lenka Dulovicova, Product Program Manager, UiPath
JMeter webinar - integration with InfluxDB and GrafanaRTTS
Watch this recorded webinar about real-time monitoring of application performance. See how to integrate Apache JMeter, the open-source leader in performance testing, with InfluxDB, the open-source time-series database, and Grafana, the open-source analytics and visualization application.
In this webinar, we will review the benefits of leveraging InfluxDB and Grafana when executing load tests and demonstrate how these tools are used to visualize performance metrics.
Length: 30 minutes
Session Overview
-------------------------------------------
During this webinar, we will cover the following topics while demonstrating the integrations of JMeter, InfluxDB and Grafana:
- What out-of-the-box solutions are available for real-time monitoring JMeter tests?
- What are the benefits of integrating InfluxDB and Grafana into the load testing stack?
- Which features are provided by Grafana?
- Demonstration of InfluxDB and Grafana using a practice web application
To view the webinar recording, go to:
https://www.rttsweb.com/jmeter-integration-webinar
UiPath Test Automation using UiPath Test Suite series, part 3DianaGray10
Welcome to UiPath Test Automation using UiPath Test Suite series part 3. In this session, we will cover desktop automation along with UI automation.
Topics covered:
UI automation Introduction,
UI automation Sample
Desktop automation flow
Pradeep Chinnala, Senior Consultant Automation Developer @WonderBotz and UiPath MVP
Deepak Rai, Automation Practice Lead, Boundaryless Group and UiPath MVP
2. Beta Lactamase inhibitor sulbactum is beta lactum structure that have
Negligible antibacterial activity but inhibit beta lactamases.
Sulbactum can be administered alongside penicillins to protect them from
Beta lactamases and to broaden their spectrum of activity.
Betalactamase inhibitors are
Clavulanic acid
Tazobactum
3.
4.
5.
6.
7. *Sulbactam sodium is a derivative of the basic penicillin nucleus.
Sulbactam is a sulfone of penicillanic acid, is synthesized from 6-APA .
Both compounds have extremely weak antibacterial properties and act by forming
irreversible complexes with beta-lactamase, which inactivates the enzyme, and as a
result the beta-lactam antibiotic has time to destroy the microorganism.
*Sulbactam is a molecule that is given in combination with beta-
lactam antibiotics to inhibit beta-lactamase, an enzyme produced by
bacteria that destroys the antibiotics.
*Chemically, sulbactam sodium is sodium penicillinate sulfone;
sodium (2S, 5R)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
4,4-dioxide.
*Its chemical formula is C8H10NNaO5S
*molecular weight of 255.22.
*The structural formula of
sulbactum is:
Chemistry of sulbactum:
8. No acylamino side chain at
6th position
Beta lactum ring
Free corboxylate essentialBicyclic system
Is important
Sulbactum mechanism is based on irreversible inhibitor and could be classed as a
Suicide substrate.
The drug fits the active site of betalactamase, and the beta lactum ring is opened by
Serine residue . The acyl-enzyme intermediate then reacts further with another enzymatic
Nucleophilic group(possibly NH2 ) to bind the drug irreversibly to the enzyme.
Sulfone group is essential and also
Enhances the activity.
The corbonyl on the
Betalactum at position -7 is must
N at position 1
Is must for activity.
Methyl groups at
Position 3 are required
For activty.
SAR (structure activity relationship )of Sulbactum
9. Structure activity relation ship (SAR)of Sulbactum:
1. Beta lactum ring(tetracyclic amide) is essential for the activity.
2.Any modifications result in an inactive compound.
3.Oxidation of sulphur to sulfone enchaces the activity.
4.Removal of oxygen atom from 4th position may result an inactive compound.
5.In sulbactum removal or substitution of hetero N atom by any other hetero atom
results in an inactive compound.
6.Removal of ketone bonds results in a new compound with reduced activity
or devoied of any activity.
7.Sulbactum should irreversibly bind with enzyme and inactivate it.
Rate and extent of formation of inhibitor-enzyme complex determines the potency.
-
13. Most beta lactamases and as such is now used in combination with traditional
Pencillins such as amoxicillin(+ Clavulanic acid Augmentin)
This allows the dose levels of amoxicillin to be decreased and also increases the
Spectrum of activity.
The sulbactum is beta lactamase inhibitor, it act as suicide substrates for
Beta lactamase enzymes .
Sulbactum has a broader spectrum of activity against betalactamases than
Clavulanic acid but is less potent.
Sulbactum is combined with ampicillin for I.V (intravenous administration in a
Preparation called Unasyn.
Tazobactum is similar to sulbactum ,How ever its potency is more like clavulanic acid
It is administeted intravenously with piperacillin in a preparation called
Tazocin or Zosyn.
Sulbactum+ ampicillin = Unasyn.
Clavulanic acid+amoxycillin = Augmentin.
Tazobactumz+pieracillin = Tazocin or Zosyn.