Medicinal Chemistry

By Prof. Harinath Chakrapani | IISER Pune

Learners enrolled: 3872

The main objective of this course is to familiarize students with the fundamental concepts of drug discovery and development. The course is intended for students who have a background in chemistry and interested in the process of drug discovery. The intended outcome is to train students on various aspects of new drug discovery/development, drug screening, target identification, lead discovery, optimization and the molecular basis of drug design and drug action.

INTENDED AUDIENCE : Third year undergraduates of B.Sc. Chemistry; M.Sc. Chemistry students and doctoral students

PREREQUISITES : Any student who has done basic organic chemistry and has some knowledge of biochemistry with an interest in drug discovery

INDUSTRY SUPPORT : Companies in the pharmaceutical sector may recognize and value this course.

Summary

Course Status :	Completed
Course Type :	Core
Duration :	12 weeks
Category :	Chemistry
Credit Points :	3
Level :	Undergraduate/Postgraduate
Start Date :	27 Jan 2020
End Date :	17 Apr 2020
Enrollment Ends :	03 Feb 2020
Exam Date :	25 Apr 2020 IST

Note: This exam date is subjected to change based on seat availability. You can check final exam date on your hall ticket.

Page Visits

Course layout

Week 1  : An overview of drugs and drug targets; structure of a cell; intermolecular binding forces; classification of drugs.
Week 2  : Principles of enzyme structure, catalysis and inhibition in drug discovery: Enzyme mechanisms overview; enzyme catalysis and inhibition in drug discovery; reversible and irreversible inhibitors; transition-state inhibitors; case studies
Week 3  : Principles of enzyme structure, catalysis and inhibition in drug discovery: Enzyme mechanisms overview; enzyme catalysis and inhibition in drug discovery; reversible and irreversible inhibitors; transition-state inhibitors; case studies,Receptors function and ligand binding interactions; Ion channel receptors; kinase-linked receptors; G-Protein coupled receptors, drug-receptor interaction; dose-response curves; case studies
Week 4  : Receptors function and ligand binding interactions; Ion channel receptors; kinase-linked receptors; G-Protein coupled receptors, drug-receptor interaction; dose-response curves; case studies
Week 5  : Nucleic acids structure and function; DNA Interactive agents and chemotherapy: DNA binding agents; intercalation and alkylation; DNA strand breakers; case studies
Week 6  : Synthetic methods in medicinal chemistry: Combinatorial and parallel synthesis: solid phase techniques, mix and split method in combinatorial synthesis; dynamic combinatorial synthesis; solid phase synthesis; diversity-oriented synthesis.
Week 7  : Lead discovery; Bioassays; drug targets; Lead Modification; optimization; pharmacophore; homologation; bioisostere; chain branching; Electronic effects; Lipophilicity; Structure-Activity Relationships; Quantiative-structure activity relationships (QSAR).
Week 8  : Lead discovery; Bioassays; drug targets; Lead Modification; optimization; pharmacophore; homologation; bioisostere; chain branching; Electronic effects; Lipophilicity; Structure-Activity Relationships; Quantiative-structure activity relationships (QSAR).
Week 9  : Drug metabolism and pharmacology: Analytical methods in metabolism; Phase I and Phase II transformations; Absorption, distribution, metabolism and excretion (ADME); bioavailability; pre-clinical and clinical development; therapeutic index and therapeutic window.
Week 10  : Prodrugs and drug delivery systems: Use of prodrug systems; prodrugs for stability, solubility and slow release; overview of drug delivery
Week 11  : Drug resistance mechanisms and synergism: Mechanisms of drug resistance; circumventing drug resistance; drug synergy
Week 12  : Drug resistance mechanisms and synergism: Mechanisms of drug resistance; circumventing drug resistance; drug synergy

Books and references

An Introduction to Medicinal Chemistry, Graham L. Patrick; Second Edition.The Organic Chemistry of Drug Design and Drug Action, Richard B. Silverman, Second EditionLehninger’s Principles of Biochemistry, Cox and Nelson, Fifth Edition (Reference).

Instructor bio

Prof. Harinath Chakrapani

IISER Pune

Prof. Harinath Chakrapani completed his undergraduate and post-graduate studies in Chemistry from Loyola College and Indian Institute of Technology Madras, respectively. He moved to Duke University, USA to pursue his doctoral studies and after post-doctoral research stints at Wake Forest University and the National Cancer Institute, USA, he joined IISER Pune in July 2009 and is currently Associate Professor. His research interests are in organic chemistry and chemical biology. His laboratory works on developing new tools to study effects of oxidative stress responses in cells and antibiotic resistance. He has over eight years of teaching experience at IISER Pune.

Course certificate

• The course is free to enroll and learn from. But if you want a certificate, you have to register and write the proctored exam conducted by us in person at any of the designated exam centres.
• The exam is optional for a fee of Rs 1000/- (Rupees one thousand only).
• Date and Time of Exams: 25th April 2020, Morning session 9am to 12 noon; Afternoon Session 2pm to 5pm.
• Registration url: Announcements will be made when the registration form is open for registrations.
• The online registration form has to be filled and the certification exam fee needs to be paid. More details will be made available when the exam registration form is published. If there are any changes, it will be mentioned then.
• Please check the form for more details on the cities where the exams will be held, the conditions you agree to when you fill the form etc.

CRITERIA TO GET A CERTIFICATE:
• Average assignment score = 25% of average of best 8 assignments out of the total 12 assignments given in the course.
• Exam score = 75% of the proctored certification exam score out of 100
• Final score = Average assignment score + Exam score

YOU WILL BE ELIGIBLE FOR A CERTIFICATE ONLY IF AVERAGE ASSIGNMENT SCORE >=10/25 AND EXAM SCORE >= 30/75.
• If one of the 2 criteria is not met, you will not get the certificate even if the Final score >= 40/100.
• Certificate will have your name, photograph and the score in the final exam with the breakup.It will have the logos of NPTEL and IIT Madras. It will be e-verifiable at nptel.ac.in/noc.
• Only the e-certificate will be made available. Hard copies will not be dispatched.

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