Course Identification

Chemistry module: Introduction to medicinal chemistry
20186172

Lecturers and Teaching Assistants

Prof. Abraham Nudelman, Ms. Vardit Berger
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Course Schedule and Location

2018
Second Semester
Tuesday, 09:00 - 11:00, San Martin, seminar room

Tutorials
Tuesday, 11:00 - 12:30, San Martin, seminar room
20/03/2018

Field of Study, Course Type and Credit Points

Science Teaching (non thesis MSc Track): Lecture; Obligatory; 2.00 points

Comments

N/A

Prerequisites

N/A

Restrictions

20
For students in the Rothschild-Weizmann program only

Language of Instruction

Hebrew

Attendance and participation

Required in at least 80% of the lectures

Grade Type

Numerical (out of 100)

Grade Breakdown (in %)

100%

Evaluation Type

Final assignment

Scheduled date 1

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-
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Estimated Weekly Independent Workload (in hours)

6

Syllabus

The main goal of the course is to introduce the students to basic terminology of medicinal chemistry and drugs development. Particular emphasis will be placed on the description of the mechanisms by which various drugs work.

Introduction

a) Drugs
b) Receptors: General considerations
c) Stereochemistry
d) Structure Activity Relationships (SAR's)
e) Absorption, Distribution and Elimination of Drugs
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, beta-Lactamase Inhibitors
2) Vancomycin
3) Tetracyclines


AnticancerAgents

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) Anti-estrogens­ Tamoxifen and anti-androgens
6) Miscellaneous Antitumor Agents: Etoposide, Taxol
7) Bisphosphonates


Anesthetics

a) General
b) Local


Hypnotics and Sedatives

a) Alcohol
b) Barbiturates
c) Benzodiazepines


Neuropharmacological Agents

a) Adrenergics: Epi, Nor-Epi, Isoproterenol, metaproterenol, salbutamol
b) Amphetamines and Anorexics
c) Stumulants
d) Artificial Sweeteners

  1) Saccharin
  2) Maltitol, xylitol
  3) Acesulfame K
  4) Cyclamates
  5) Aspartame
  6) Sucralose

e) Cholinergics and Anticholinesterases
f) Choline esterase inhibitors - Nerve Gases
g) Cholinesterase Reactivators


Histamine H-1 and H-2 Antihistamines    Prazoles


Analgesics

1) Salicylates - Aspirin
2) Fenamates
3) Indomethacin and Congeners
4) Phenyl Propionic Acids
5) Enolic and other Acidic Agents
6) New agents: COX2 Inhibitors


Thyroid Hormones  T3 and T4


Topical Drugs
1) Sun blockers


Hormones and Steroids.
1) Gluco- and Mineralo-corticoids ­ Cortisone
2) Estrogens and Progestins. The Pill.
3) Antiestrogens
4) Aromatase inhibitors
5) Androgens - DHT inhibitors
6) Viagra


Cardiovascular Drugs
a) Nitrites and Nitrates - Nitroglycerine
b) beta-Blockers - Propranolol
c) Calcium-Blockers ­ Dihydropyridines, Diltiazem, Verapamil


Antihypertensive Agents

1) ACE inhibitors ­ ³Prils²
2) Angiotensin II inhibitors ³Sartans²
3) Drugsaffecting the Nor-Epi pathway


Cholesterol - HMG-CoA-Reductase inhibitors: ³Statins²


Major Analgesics

1) Morphinoids: Morphine, Heroin
2) Antitussive Agents - Codeine
3)Enkephalins and Endorphins
4) Cannabinoids: THC


Suntan lotions

Antimicrobial Agents and Antibiotics -

1) Sulfanilamides
2) Fluoroquinolones
3) Miscellaneous Antibiotics
4) Bacterial resistance


Antipsychotic Agents

a) Tricyclic Antidepressants - Chlorpromazine
b) Non-Tricyclic Antidepressants
c) Prozac
d) Antischizophrenics


Antifungal agents

Learning Outcomes

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

  1. Demonstrate a proficiency in a large variety of drugs and recognize their clinical use from their basic structures and names.
  2. [Describe drugs mechanisms of action by which the drugs act, 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

Website

N/A