Thrombin inhibitors. 3. Carboxyl-containing amide derivatives of N. alpha.-substituted L-arginine

…, S Tonomura, S Okamoto, A Hijikata

Index: Kikumoto; Tamao; Ohkubo; Tezuka; Tonomura; Okamoto; Hijikata Journal of medicinal chemistry, 1980 , vol. 23, # 12 p. 1293 - 1299

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Citation Number: 47

Abstract

A series of N"-(arylsulfonyl)-L-arginine amide derivatives having carboxamide N- substituents with a carboxyl group was prepared and tested as inhibitors of the clotting activity of thrombin. The most inhibitory compounds were obtained when a carboxyl group was introduced into the carbon next to the amide nitrogen of Nu-(arylsulfonyl)-L-arginine amide derivatives, eg, N'-(arylsulfonyl)-L-arginyl-N-butyl-, N-(methoxyethy1)-or N-( ...