Antianginal Drugs_ Medicinal Chemistry Perspective

Antianginal Drugs: Medicinal Chemistry Perspective

Slide 1: Introduction to Antianginal Drugs

Definition and brief overview

Importance in cardiovascular medicine

Slide 2: Classes of Antianginal Drugs

Organic Nitrates

Beta-Adrenergic Blockers

Calcium Channel Blockers

Novel Agents

Slide 3: Organic Nitrates

Chemical structures: Nitroglycerin, Isosorbide mononitrate, Isosorbide dinitrate

Structure-Activity Relationships (SAR)

Mechanism: NO donors 鈫?Vasodilation

Metabolism and bioactivation

Slide 4: Beta-Adrenergic Blockers

General structure and key functional groups

Examples: Propranolol, Metoprolol, Atenolol

SAR: Cardioselectivity (尾1 vs. 尾2)

Stereochemistry and its importance

Slide 5: Calcium Channel Blockers

Chemical classes:

Dihydropyridines (e.g., Nifedipine, Amlodipine)

Phenylalkylamines (e.g., Verapamil)

Benzothiazepines (e.g., Diltiazem)

SAR for each class

Binding site interactions

Slide 6: Novel Antianginal Agents

Ranolazine

Chemical structure and properties

SAR for late sodium current inhibition

Ivabradine

Unique structure and selectivity for If channels

SAR for If channel binding

Slide 7: Pharmacophores

Key structural features for each drug class

Comparison of pharmacophores across classes

Slide 8: Drug Design Strategies

Rational drug design approaches

Computational methods in antianginal drug discovery

Lead optimization techniques

Slide 9: Prodrug Approaches

Nitrate esters as prodrugs

Other prodrug strategies in antianginal therapy

Slide 10: Synthetic Routes

Key synthetic pathways for major antianginal drugs

Industrial synthesis considerations

Slide 11: Structure-Based Drug Design

Crystal structures of drug targets (e.g.