The main goal of the course is to introduce the students to the 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 – 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, beta-Lactamase Inhibitors
2) Vancomycin
Anticancer Agents
1) Alkylating Agents: N-Mustards, Nitrosoureas, Pt complexes, Mitomycin
2) Antimetabolites: 5-FU, Methotrexate, Ara-C, Mercaptopurine
3) Intercalators: Actinomycin D, Adriamycin, and Daunomycin
4) Epothilones
5) Antiestrogens – Tamoxifen
6) Miscellaneous Antitumor Agents: Etoposide, Taxol
7) Bisphosphonates
Anesthetics
a) General
b) Local
Hypnotics and Sedatives
a) Alcohol
b) Barbiturates
c) Benzodiazepines
d) Drugs of abuse
Neuropharmacological Agents
a) Adrenergics: Epinephrine, norepinephrine, 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
Prazoles
Analgesics
1) Salicylates - Aspirin
2) Fenamates
3) Indomethacin
4) Phenyl propionic Acids
5) Enolic and other acidic agents
6) Cyclooxygenase (COX) inhibitors
Antifungal Agents
Ergosterol inhibitors
Amphotericin B
Diazoles, triazoles
Podophyllotoxin
Xanthines
Caffeine, theophylline, theobromine
Thyroid Hormones
T3 and T4
Topical Drugs
1) Sun blockers
2) Insect repellants
3) 5-Aminolevulinic acid photodynamic therapy (PDT)
Hormones and Steroids.
1) Gluco- and mineralocorticoids – Cortisone
2) Estrogens and progestins. The Pill.
3) Antiestrogens
4) Aromatase inhibitors
5) Bisphosphonates
6) Androgens - DHT inhibitors
7) 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
Antilipidemic and Anticholesterolemic agents: Vile acid sequestrants, Gemfibrozil
HMG-CoA-Reductase inhibitors: “Statins”
Major Analgesics
1) Morphinoids: Morphine, Heroin
2) Antitussive Agents - Codeine
3) Enkephalins and Endorphins
4) Cannabinoids: tetrahydrocannabinol (THC), cannabidiol
Antimicrobial Agents and Antibiotics
1. Sulfanilamides
2. Fluoroquinolones
3. Miscellaneous Antibiotics
4. Linezolid
5. Bacterial resistance
Antiepileptics
a) Phenytoin
b) Valproic acid
b) Valproic acid
Antipsychotic Agents
a) Tricyclic antidepressants – Typical and atypical antipsychotics
b) Non-Tricyclic antidepressants
c) Prozac
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
14) ADEPT
15) Ring-opened PD's
16) Mutual PD's
17) Multi-pharmacophores