MEDICINAL CHEMISTRY

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Official drugs: Propranolol Hydrochloride, B.P., I.P. (RS)-1-Isopropylamino-3-(1-naphthyloxy)propan-2-ol hydrochloride. Propranolol hydrochloride is a white or almost white powder. It is soluble in water. Propranolol is highly lipophilic and is almost completely absorbed from the gastrointestinal tract. Propranolol is extensively metabolized in the liver with most metabolites appearing in the urine. The major metabolite is the carboxylic acid. One product of hepatic metabolism is 4- hydroxy propranolol (54) which possesses some adrenergic blocking activity. Propranolol is used in the treatment of hypertension, to improve the tolerance to exercise in patients with angina pectoris, and has been given for the prevention of reinfarction in patient who has suffered an acute myocardial infarction. It is also used in the treatment of cardiac arrhythmias. It is often effective in supraventricular tachyarrhythmia. The dose of the drug is 20 mg to 2 g daily, in divided doses, the initial daily dose not to exceed 40 mg; and by slow intravenous injection the dose is 3 to 10 mg. Preparations: Propranolol Injection, B.P. Propranolol Tablets, B.P., I.P. Proprietary Names: CARDIOLONG; INDERAL; IPRAN A (3). α, β - adrenoceptor antagonists: e.g. Labetalol CH 2-CH 2-CH-NH-CH 2-CH CH 3 Labetalol (60) OH CONH 2 It possesses two chiral centers and therefore is administered as a mixture of four stereoisomers, of which R(CH3), R(OH) is the active β-blocker and the S(CH3), R(OH) diastereomer is predominantly an α1-blocker. R, R diastereomer of labetalol also known as dilevalol. S(CH3), S(OH) and R(CH3), S(OH) diastereomer are both inactive Official drug: Labetalol Hydrochloride, B.P. all-rac-2-Hyhydroxy-5[1-Hydroxy-2-(1--methyl-3phenylpropylanmo)- ethyl]-benzamide hydrochloride. Labetalol hydrochloride forms white powder or granules. It is sparingly soluble a water. Labetalol is readily absorbed from the gastrointestinal tract. The metabolites are excreted in the urine along with only small amounts of unchanged Labetalol. Labetalol is a nonselective β-blocker that acts as a competitive antagonist at both α1- and β-adrenergic receptors. Labetalol decreases blood pressure more rapidly than other β-blockers. Labetalol hydrochloride is usually given by mouth in the OH
treatment of hypertension, the dosage varying from 200 mg to 2.4 g daily in divided doses. Preparations: Labetalol Injection, B.P. Labetalol Tablets, B.P. Proprietary Names: NORMADATE; NORMODYNE; TRANDATE, A (4). Centrally Acting Agents HO CH 3 HO CH 2 C COOH Methyldopa (61) Cl Cl CH=NNC Guanabenz (63) NH NH 2 NH 2 H N Cl Cl N NH Cl Cl Clonidine (62) O CH 2CNHC Guanfacine (64) α-Methyldopa (61) is converted into α-methyl noradrenaline which acts as a false neurotransmitter which activates central α-receptor and produce fall in blood pressure. Clonidine (62) originally developed as nasal decongestant. It is also used in the treatment of all grades of hypertension. There are two major metabolites of clonidine are phydroxyclonidine (65) and its O-glucuronide. H N N NH OH p-Hydroxyclonidine (65) Synthesis of Methyldopa: Cl Cl NH NH 2
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: Official drugs: Prazosin Hydrochlor
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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