MEDICINAL CHEMISTRY

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+ + N (CH2) 5 N CH 3 H 3C Pentolinium (74) Synthesis of Mecamylamine: CH 3 Camphene (77) LiAl(H) 4 CH 3 + S + Hydrocyanic Acid Mecamylamine (76) H 2C N N H 2C Trimethaphan (75) Strong Acid O NHCHO CH 3 CH 3 CH 3 3-formamidoisocamphane (78) NHCH 3 CH 3 CH 3 CH 3 Mecamylamine (76) Official Drug Mecamylamine Hydrochloride, I.P. Methyl-2, 3, 3-trimethylbicyclo-[2, 3, 3]-hept-2-ylamine hydrochloride. Mecamylamine hydrochloride is a white crystalline powder. It is soluble in water. It is almost completely absorbed from the gastrointestinal tract. It is excreted slowly by the kidney in unchanged form and has a relatively long duration of action. Mecamylamine hydrochloride may be indicated in severe or malignant hypertension. It is available as tablets for oral administration. The initial dosage is 5 mg daily, in divided doses; the subsequent doses are in accordance with the needs of the patients. Proprietary Name: INVERSIVE B(1). Angiotensin Converting Enzyme (ACE) Inhibitors:Captopril (79), Enalapril (80) is prodrug that is not itself highly active and it must be hydrolyzed to enalaprilate. Lisinopril (81) is the lysine analogue of enalaprilate and is itself active. HS H CH 3 O N Captopril (79) H COOH H H N O H CH3 COOC 2H5 Enalapril (80) N H COOH
B (2). Angiotensin Receptor Antagonist C(1)a. Directly Acting Vasodilators: N H N N NHNH 2 N N Hydralazine (84) Synthesis of Hydralazine: N H H N H COOH R R=CH2CH2CH2CH2NH2 O N Lisinopril (81) Sar-Arg-Val-Tyr-Val-His-Pro-Ala Saralasin (82) N NC NC NC N OH Cl Losartan (83) CN Fe NO, CN Nitroprusside sodium (85) H COOH -2 2Na +
Page 1 and 2: CONTENTS Antianginal Drugs Anticoag
Page 3 and 4: c) Dihydropyridine derivative: e.g.
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: NH ClCH 2CN NCH 2CN Perhydroazocine
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

MEDICINAL CHEMISTRY

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