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An-Najah National University
College of medicine and health sciences
Department of Pharmacy
Medicinal chemistry 1 (7303301)
First semester 2013/2014
Course Description:
The aim of this course is to introduce the basic concepts of medicinal chemistry. Study
the physicochemical properties of the drugs and study their distribution, metabolism and
excretion. The course will discuss specific drug classes by covering its chemistry, some
synthesis, mechanism of action and its structural activity relationship (SAR).
Course objectives:

Recognize the relation between the drug chemical structure and its biological
activity in the body.

The importance of organic functional groups in determining the physicochemical
properties of the drug.

Understand the interactions drug-protein, drug-enzyme, and drug-receptor.

How the body interacts and makes changes on the chemical structure of the drug.

Introduce various classes of therapeutic agents with the emphasis on their
structure activity relationship (SAR).
Intended learning outcomes (ILOs):
a. Knowledge and understanding:
a.1
Recognise and identify drug receptor, drug enzyme, drug protein
interactions
a.2
Be familiar with the main classification of drugs
a.3
Describe the physicochemical properties of drugs and its roll in drugs
absorption to blood circulation and crossing of system barriers
a.4
Identify The Henderson-Hasselbalch Equation in calculating the drug
ionization and its effect on drug absorption
a.5
Describe importance of water solubility of drug and relate it to its
chemical structure.
a.6
Define the biological factors that affect the drug metabolism
a.7
Define the different phases of drug metabolism in the body (phase I and
phase II) with their different chemical modifications.
a.8
Describe the SAR of different types and classes of drugs
b. Intellectual Skills:
b.1
Differentiate between drug as an enzyme substrate and its action on a cell
receptor
b.2
Differentiate between ionisable and non ionisable drug functional group
b.3
Recognise the hydrophilic and lipophilic properties of the drug chemical
structure.
b.4
Differentiate between the general chemical reaction involved in Phase I
and Phase II drug metabolism.
b.5
Recognise the medicinal action of chemical compounds according to their
structure.
c. Professional and practical skills:
c.1
Be able to propose new drug chemical structure to modify drug activity
c.2
Be able to resolve problems related to drug solubility and absorbtivity in
mammalian system
c.3
Be able propose chemical modifications to different types of drug
formulations
d. General and transferable skills:
Search the internet database for current chemical modification of newly developed
d.1
antibacterial, anti-infective drugs and Non-Steroidal Anti-Inflammatory drugs
(NSAIDs)
d.2
Independent learning through literature searching and presenting work.
d.3
Appreciate team work in the seminar
d.4
Work in a team
d.5
Respect assisting personal.
Course Outline:
Topics
Week/ hours
Chapter I: Introduction to medicinal chemistry

History of medicinal chemistry

Drug Discovery

General Classification of drugs
1.5hours
Chapter II: Introduction of drug targets

Cell structure

Cell membrane

Drug targets

Intermolecular bonding forces
1.5hours
Chapter III: Proteins as drug targets

The building blocks of protein and their structure

Protein function
1.5hours
Chapter IV: Enzymes as drug targets

Overall Process of Enzyme Catalysis

Enzyme targets for useful medications
1.5hours
Chapter V: Receptors as drug targets

Receptor function

Messenger binding

Overall Process of Receptor/Messenger Interaction

Design of Agonists

Design of Antagonists
2hours
Chapter VI: Review of important functional groups.

Nitrogen Containing Functional Groups.

Oxygen Containing Functional Groups

Aromatic Hydrocarbons

Heterocycles
5hours
Chapter VII: Pharmacokinetic of drugs
a. Drug absorption & distribution

Ionisation of Drug Molecules

Drug Partition coefficient

Solubility of Drugs

Distribution
b. Drug metabolism & Excretion

Biological factors affecting metabolism

Pharmacological effect of metabolism on drugs

Phase I metabolic reactions

Phase II metabolic reaction or conjugation reaction

excretion
10hours
Chapter VIII: Anti-infective drugs:

Desinfectants & antiseptics

Antifungal

Antiprotozoal Agents

Anthelmintics

Antimalarial
7hours
Chapter IX: Antibacterial agent

Antibacterial agents which act against cell metabolism

Antibacterial agents which inhibit cell wall synthesis

Antibacterial agents which act on the plasma membrane
structure

9 hours
Antibacterial agents which impair protein synthesis:
translation

Agents which act on nucleic acid: transcription and
replication
Chapter X: Antiviral agent

Structure & life cycle of viruses

Antiviral drugs used against DNA viruses

Antiviral drugs acting against RNA viruses: HIV

Antiviral drugs Agents for the treatment of influenza
5hours
Chapter XI: Nonsteroidal Anti-inflammatory Drugs
“NSAIDS”

Classes of COX inhibitors

The COX binding site

The salicylates

Fenemates

p-Aminophenols

Arylacetic acid derivatives

Arylpropioanic acid derivatives

Oxicams

Miscellaneous
Total hours
4hours
48
Text Books:
-
Foye's principles of medicinal chemistry, Williams DA and Lemke TL, Sixth
edition. 2008, Lippincott Williams & Wilkins
-
An Introduction to Medicinal Chemistry by Graham L. Patrick, fifth edition.2013,
Oxford University Press, USA;
-
Textbook of organic medicinal and pharmaceutical chemistry, by Wilson and
Gisvold's, Eleventh edition. Lippincott Williams & Wilkins, 2011.
Medicinal Chemistry Gareth Thomas, Second Edition ,Wiley, 2007.
-
Medicinal chemistry by Ashtush Kar- fourth edition. New Age International, 2007.
-
Grades:
1st Exam: 20%.....2/10/2013 “Wednesday”
2nd Exam: 20%.....11/11/2013 “Moneday”
Quizes, participation & attendance: 10%
Presentation: 10%
Final Exam: 40%