MEDICINAL CHEMISTRY

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NH H 2N C NH (CH 2) n NH HN C NH 2 Synthalin A (202) ; decamethylene; n=10 Synthalin B (203) ; dodecamethylene; n=12 Biguanides also reduce the GIT absorption of amino acids and other ingredients of dietary energy value. They also lower the plasma levels of triglycerides and cholesterol. In the treatment of maturity onset diabetes, biguanides thus offer two fold advantage. They induce weight loss and reduce obesity along with their hypoglycemic action. In patients with cardiac (myocardial infarction) or renal disease, phenformin treatment was found to increase blood lactic acid level. This lactic acidosis sometimes induces severe fatalities in patients. Lactic acidosis is characterized by dehydration, acidosis and a bicarbonate deficiency. This complication demands contraindication of phenformin in patients having liver, heart and kidney diseases. Along with acidosis, prolonged use of phenformin is found to induce malabsorption of cyanocobalamin. On the creditable sides, biguanides sometime have been used in combination with insulin preparation for smoother control of brittle diabetes in some patients. They are also used in combination with sulfonylureas, in cases where treatment with either agent alone, fails. Mechanism of Action: The mechanism of action include- • Inhibition of intestinal transport and absorption of sugars. • Inhibition of hepatic gluconeogenesis potentiation of action of insulin on glucose transport process into cell. • Enhancement of glucose utilisation process. e.g. Synthalin A; Decamethylene (H=10) Synthalin B: Dodecamethylene (H=12) b) First, Second and Third Generation Sulfonylureas 1 st Generation 2 nd Generation 3 rd Generation Tolbutamide Glyburide (Glibenclamide) Glybormuride Chlorpropamide Glipizide Glypizide Tolazamide Glimepirides Acetohexamide Repaglinide The clinically used sulfonylureas are represented above. In all effective compounds, a substituted aryl sulfonyl moiety is attached to N 1 of urea molecule. These derivatives are structurally similar and bear essentially the similar properties. They differ in their duration of action and chemically in the nature of the substituent at para position (-X-) and R. The substitution of aliphatic side-chain present in the first generation hypoglycemic sulfonylurea by cyclopentyl or cyclohexyl group and addition of yet another ring structure to the aromatic nucleus resulted into development of more potent second generation series.
Key to general structure X SO 2 NH C (204) O NH Y Name 1 X Y st Generation Tolbutamide (205) Chlorpropamide (206) CH3 Cl -(CH2) 3-CH3 -(CH2) 3-CH3 Acetohexamide (207) CH 3C O Tolazamide (208) CH 3 N Carbutamide (209) 2 NH2 (CH2) 2 CH3 nd Generation Cl Glibenclamide (210) OCH 3 Glymide (211) SO 2 NH Glypentide (212) OCH 3 CONH(CH 2) 2 CONHCH 2CH 2 Glycodiazine (213) SO 2 NH N N N N CH 2 CH 2OCH 3 SO 2NHCONH OCH 2CH 2OCH 3
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CONTENTS Antianginal Drugs Anticoag
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c) Dihydropyridine derivative: e.g.
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2 (d) 4. H 3C H 3C HO CH-CH 2-O-CH
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pentaerythritol, and is supplied di
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of' streptokinase, urokinase and ti
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Low-molecular-weight Heparins, B.P.
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OH COOCH 3 AC 2O Methyl salicylate
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Warfarin and other coumarin derivat
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Structure-activity Relationship All
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Mean Arterial Blood Pressure (MABP)
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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: for better drug in this series. Sub
Page 77 and 78: Official Drugs: Insulin, B.P. It is
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MEDICINAL CHEMISTRY

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