MEDICINAL CHEMISTRY

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1. Antianginal Drugs Introduction The word ‘angina’ derived form the Greek verb meaning to choke and is used to describe the pain or discomfort. Angina occurs when the blood supply to the heart is not able to meet the metabolic demands of the heart for oxygen. Angina pectoris, or ischemic heart diseases, is the name to the symptomatic oppressive pain resulting from myocardial ischemia. An angina may have typical and variant forms, both of which may result in sudden, severe, pressing substantial pain, radiating to the left shoulder and along the flexor surface of the left arm. In typical angina the pain is generally induced by exercise, emotion, or eating. The variant (Prinzmetal’s) angina on the other hand is caused by vasospasm of the coronary vessels and may not be associated with severe atherosclerosis (Fig.1). Cardiac CHEST PAIN Non-cardiac Ischemia Non-ischemic Pulmonary Gastrointestinal - Coronary - Pericarditis atherosclerosis (Esophagial spasm) - Aortic dissection - Coronary spasm - Cardiomyopathies Psychogenic - Depression - Anxiety Fig.: Kinds of Pain Neuromusculoskeletal The antianginal drugs are directed mainly to alleviating and preventing anginal attacks by dilating the coronary artery. Classification of Antianginal drugs 1) Nitrates and nitrites a) Nitrates: e.g. Nitroglycerin (1), Erythritol tetranitrate (2), Trolnitrate phosphate (3), Isosorbide dinitrate (4), Pentaerythritol tetranitrate (5), Mannitol hexanitrate (6). b) Nitrites: e.g. Amyl nitrite (7), Sodium nitrite (8), Nitroprusside sodium (9). 2) Calcium Channel Blockers a) Aryl alkyl amine derivative: e.g. Verapamil (10) b) Benzothiazepine: e.g. Diltiazem (11)
c) Dihydropyridine derivative: e.g. Nifedipine (12), Nimodipine (13), Nitrendipine (14), Nicardipine (15), Amlodipine (16), Felodipine (17), Isradipine (18). d) Newer second generation alkyl amine derivative: e.g. Bepridil (19) 3) β-Adrenergic Antagonist: e.g. Propranolol (see antihypertensives) 4) Miscellaneous Coronary Vasodilators: e.g. Dipyridamol (20), Cyclandelate (21), Papaverine (22) Structures of some Anti-anginal Drugs 1 (a) 1 (b) CH 2ONO 2 CHONO 2 CH 2ONO 2 Nitroglycerin (1) N CH 2CH 2ONO 2 CH 2CH 2ONO 2 .H3PO 4 CH2CH2ONO2 Trolnitrate Phosphate (3) O 2NOH 2C CH 3-CHCH 2CH 2ONO CH 3 Amyl nitrite (7) CH 2ONO 2 C CH 2ONO 2 CH 2 CH O O2NOCH CH 2ONO 2 Pentaerythritol tetranitrate (5) NaONO Sodium Nitrite (8) CHONO2 O CH2 CH 2 Isosorbide dinitrate (4) CH 2ONO 2 CHONO 2 CHONO 2 CH 2ONO 2 Erythritol tetranitrate (2) O 2NO O 2NO CH2ONO 2 CH CH CHONO 2 CHONO 2 CH2ONO2 Mannitol hexanitrate (6) NC NC NC CN Fe NO 2Na + CN -2 Nitroprusside sodium (9)
Page 1: CONTENTS Antianginal Drugs Anticoag
Page 5 and 6: 2 (d) 4. H 3C H 3C HO CH-CH 2-O-CH
Page 7 and 8: pentaerythritol, and is supplied di
Page 9 and 10: of' streptokinase, urokinase and ti
Page 11 and 12: Low-molecular-weight Heparins, B.P.
Page 13 and 14: OH COOCH 3 AC 2O Methyl salicylate
Page 15 and 16: Warfarin and other coumarin derivat
Page 17 and 18: Structure-activity Relationship All
Page 19 and 20: Mean Arterial Blood Pressure (MABP)
Page 21 and 22: Table-1 ---------------------------
Page 23 and 24: Ramipril Altace ( Hoechst-Marion) 2
Page 25 and 26: Official drugs: Prazosin Hydrochlor
Page 27 and 28: treatment of hypertension, the dosa
Page 29 and 30: NH ClCH 2CN NCH 2CN Perhydroazocine
Page 31 and 32: B (2). Angiotensin Receptor Antagon
Page 33 and 34: CH3COOC2H5 Diazoxide (90) Cl NH 2 S
Page 35 and 36: Structure-activity Relationships of
Page 37 and 38: N N R Acidic group (102) Acidic gro
Page 39 and 40: Structure-activity Relationships of
Page 41 and 42: HO HO HO HO H 3C CH 3 H Digitoxigen
Page 43 and 44: efractory periods. These are mainly
Page 45 and 46: Structure - Activity Relationship:
Page 47 and 48: Hydralazine is a direct relaxant of
Page 49 and 50: K4[Fe(CN) 6].3H2O + 6HNO3 H2[(NO)Fe
Page 51 and 52: conduction velocity, and decrease s
Page 53 and 54:
Synthesis of Moricizine: (153) H N
Page 55 and 56:
Tocainide Hydrochloride (±)-2-Amin
Page 57 and 58:
influx through β-receptor blockade
Page 59 and 60:
Cl Cl CH2CH=CH2 N N N H Alinidine (
Page 61 and 62:
(iii) Intermediate density lipoprot
Page 63 and 64:
Structure-activity Relationship Mev
Page 65 and 66:
to the bile acids. Thus due to ente
Page 67 and 68:
moderate reduction in cholesterol l
Page 69 and 70:
(iii) Other types: (a) Insulin rece
Page 71 and 72:
non-crystalline insulin as far as o
Page 73 and 74:
for better drug in this series. Sub
Page 75 and 76:
Key to general structure X SO 2 NH
Page 77 and 78:
Official Drugs: Insulin, B.P. It is
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MEDICINAL CHEMISTRY

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