Course Identification

Chemistry module: Introduction to medicinal chemistry

Lecturers and Teaching Assistants

Prof. Abraham Nudelman

Course Schedule and Location

First Semester
Tuesday, 16:30 - 18:00, FGS, Rm 2

Field of Study, Course Type and Credit Points

Science Teaching (non thesis MSc Track): Lecture; Obligatory; Regular; 4.00 points
Science Teaching: Lecture; 4.00 points


1st year + 2nd year
פורמט היברידי
No option for Zoom attendance
Three unjustified absences (such as illness) will declassify the student.


Preferable a basic course in organic chemistry


For students in the Rothschild-Weizmann program only

Language of Instruction


Attendance and participation

Required in at least 80% of the lectures

Grade Type

Numerical (out of 100)

Grade Breakdown (in %)


Evaluation Type

Final assignment

Scheduled date 1


Estimated Weekly Independent Workload (in hours)




   a) Drugs

   b) Receptors: General considerations

   c) Stereochemistry

   d) Structure Activity Relationships (SAR's)

   e) Absorption, Distribution and Elimination of Drugs – Lipinski Rules

   f) Drug Delivery through the blood brain barrier (BBB)

   g) Drug Metabolism

   h) Drug Toxicity

   i) Drug Tolerance and Addiction

   j) Pro-Drugs, Soft-Drugs and Hard-Drugs

   k) Patents in the Pharmaceutical Industry


Antimicrobial Agents and Antibiotics

  1. Penicillins, Cephalosporins, b-Lactamase Inhibitors
  2. Vancomycin
  3. Tetracyclines


Anticancer Agents

  1. Alkylating Agents: N-Mustards, Nitroso ureas, Pt complexes, Mitomycin
  2. Antimetabolites: 5-FU, Methotrexate, Ara-C, Mercaptopurine
  3. Intercalators: Actinomycin D, Adriamycin and Daunomycin
  4. Epothilone
  5. Antiestrogens – Tamoxifen
  6. Miscellaneous Antitumor Agents: Etoposide, Taxol
  7. Bisphosphonates



   a) General

   b) Local


Hypnotics and Sedatives

   a) Alcohol

   b) Barbiturates

   c) Benzodiazepines

   d) Drugs of abuse


Neuropharmacological Agents

a) Adrenergics: Epi, Nor-Epi, Isoproterenol, metaproterenol, salbutamol

b) Stimulants - Amphetamines and Anorexics

c) Artificial Sweeteners

  1) Saccharin

  2) Maltitol, xylitol

  3) Acesulfame K

  4) Cyclamates

  5) Aspartame

  6) Sucralose

d) Cholinergics and Anticholinesterases

e) Choline esterase inhibitors - Nerve Gases

f) Cholinesterase Reactivators


Histamine, H-1 and H-2 Antihistamines




   1) Salicylates - Aspirin

   2) Fenamates

   3) Indomethacin and Congeners

   4) Phenyl Propionic Acids

   5) Enolic and other Acidic Agents

   6) COX2 Inhibitors


Antiviral Agents

     Ergosterol inhibitors

     Amphotericin B

     Diazoles, triazoles




    Caffeine, theophylline, theobromine


Thyroid Hormones

    T3 and T4


Topical Drugs

  1. Sun blockers
  2. Insect repellants
  3. 5-Aminolevulinic acid PDT


Drug Delivery Systems- Prodrugs (PD's)

             1) PD's Introduction

 2) First Pass Metabolism

 3) Toxicity

 4) Hard-Drugs

 5) Ester PD's

 6) Acyloxyalkyl Ester PD's

 7) Carbamate PD's

 8) Water Solubilization via PD's

 9) Soft-Drugs

10) N-Mannic Bases

11) Amides as Amine PD's 

12) N-Hydroxymethyl PD

13) Site-specific drug delivery


15) Ring-opened PD's

16) Mutual PD's

17) Multi-pharmacophores


Hormones and Steroids.

  1. Gluco- and Mineralo-corticoids – Cortisone
  2. Estrogens and Progestins. The Pill.
  3. Antiestrogens
  1. Aromatase inhibitors
  2. Bisphosphonates
  3. Androgens - DHT inhibitors
  4. Viagra


Cardiovascular Drugs

a) Cardiac Glycosides

b) Nitrites and Nitrates - Nitroglycerine

c) b-Blockers - Propranolol

d) Calcium-Blockers – Dihydropyridines, Diltiazem, Verapamil

e) Antihypertensive Agents

  1. ACE inhibitors – “Prils”
  2. Non-peptide Angiotensin II inhibitors – “Sartans”
  3. Clonidine
  4. Drugs affecting the Nor-Epi pathway

f) Cholesterol

 1. Antilipidemic and Anticholesterolemic agents: Vile acid sequestrants, Gemfibrozil

                        2. HMG-CoA-Reductase inhibitors: “Statins”


Major Analgesics

            1) Morphinoids: Morphine, Heroin

            2) Antitussives - Codeine

            3) Enkephalins and Endorphins

            4) Cannabinoids: THC


Antimicrobial Agents and Antibiotics

  1. Sulfanilamides
  2. Fluoroquinolones
  3. Miscellaneous Antibiotics
  4. Linezolid
  5. Bacterial resistance



             a) Phenytoin

 b) Valproic acid


Antipsychotic Agents

 a) Tricyclic Antidepressants – Typical and atypical antipsychotics

 b) Non-Tricyclic Antidepressants

 c) Prozac




Learning Outcomes

Upon successful completion of the course- students should be able to:

  1. Demonstrate proficiency in a large variety of drugs and recognize their clinical use from their basic structures and names.
  2. Describe drugs' mechanisms of action, the diseases against which the compounds are used, possible side effects, and drug interactions.
  3. Explain basic principles of toxicology, structure-activity relationships, and drug design.

Reading List

List of suggested literature will be presented in the first lecture