Download FP-Overview - Philadelphia University Jordan

Medicinal Chemistry III
Module Overview
B. Pharm., Semester-1
Course Code: 0510411, Session: 2016-2017
Facilitators and Module Coordinators
DR. PRAN KISHORE DEB
DR. BILAL AL-JAIDI
Assistant Professor
Faculty of Pharmacy, Philadelphia University, Jordan
Method of Delivery
Method of Delivery
Lectures
Workshops/Tutorials
Online Quiz (Kahoot)
No. of Activities
40
05
15
2
Lecture Topics
 Anticancer agents
 Alkylating Agents
 Heavy metal compounds (Metallating Agents)
 Anti-metabolites and Antibiotics
QUIZ-1
 Plant Extracts
 Topoisomerase inhibitors
 Combination of chemotherapy with other treatments
 Diuretics
 Carbonic Anhydrase Inhibitors (CAIs)
 Loop Diuretics
QUIZ-2
 Thiazide and Thiazide-like Diuretics
 Potassium-sparing diuretics
 Osmotic diuretics
 Respiratory drug development
 Design and Development of β2- Agonists and Treatment of Asthma
 Cardiovascular drug development
 Development of β-blockers
QUIZ-3
 Calcium channel blockers
 Angiotensin converting enzyme inhibitors (ACE inhibitors)
 Angiotensin II receptor antagonists
 Direct acting vasodilator
 Gastric drug development
 Development of Proton Pump Inhibitors
No. of Lectures
15
06
03
14
02
3
Class aims, objectives and rationale
 The class relates the structure and function of various proteins,
receptors, enzymes and nucleic acids to drug discovery and action and
provides a broad overview of the drug discovery and design process.
 There is particular emphasis on the factors (potency and efficacy,
pharmacology and ADMET) that influences structure-activity
relationships (SAR) as well as guide the development of small
molecules into drug candidates and ultimately into drugs.
 Case examples from different therapeutic areas such as anti-cancer,
cardiovascular, respiratory, diuretics and anti-ulcer agents are used to
contextualise this process.
Learning outcomes:
Upon the completion of this class, the student will be able to:
 Explain how protein (receptor, enzymes) and DNA structure relates to function
with respect to their role as targets for drug discovery.
 Describe how active site topology controls specific catalytic processes that
require regulation in different therapeutic scenarios.
 Outline how multidisciplinary scientific considerations during the lead
optimisation process combine to produce a successful drug.
 Explain how knowledge of physicochemical properties in drug development can
address problems encountered with formulation, administration, absorption
and elimination.
 Describe how the requirements of drug development vary depending upon the
specific target and the therapeutic area.
 Understand how previous drugs have been successfully developed using case
studies that address varied administrative routes within a range of therapeutic
areas (for example: anti-cancer agents, cardiovascular; respiratory; diuretics).
 Show how structural modifications of drugs within these therapeutic areas can
be used to alter their pharmacodynamics and pharmacokinetics and overcome
other issues (e.g. toxicity, prodrug design).
Assessment Methods
 Formative Assessment (Practice only, Kahoot Quiz & Tutorials)
 Summative Assessment (Marks included)
Summative
Assessment
Type questions
Duration Marks
First Exam
MCQs, Fill up the blanks, SAQs
1 hr
20
Second Exam
MCQs, Fill up the blanks, SAQs
1 hr
20
Quizzes (3)
MCQs, Fill up the blanks, SAQs
1. Total 3 quizzes will be conducted.
2. Average of the three quizzes will
be considered
10 min
20
Final Exam
MCQs, SAQs, Fill up the blanks, True-False
2 hrs
40
6
100
Total
Recommended Books
1.
2.
3.
An introduction to Medicinal Chemistry by Graham L. Patrick. Fourth edition,
Oxford, 2009.
Wilson and Griswold’s Text Book of Organic Medicinal and Pharmaceutical
Chemistry by John M. Beale, Jr. and John H. Black, Twelfth edition, Lippincott
Williams and Wilkings 2011.
Foye’s principle of medicinal chemistry by David H. Williams, Thomas L. Leuke,
Williams O. Foye. Lippincot William and Wilkins. Seventh edition, 2012, ISBN. 7
Good Luck ……..
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