Dibasic benzo[B]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 4. SAR studies on the conformationally restricted C3-side chain of hydroxybenzo[B]thiophenes.

Takeuchi, K; Kohn, T J; Sall, D J; Denney, M L; McCowan, J R; Smith, G F; Gifford-Moore, D S

Takeuchi, K; Kohn, T J; Sall, D J; Denney, M L; McCowan, J R; Smith, G F; Gifford-Moore, D S.

Afiliación

Takeuchi K; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.

Bioorg Med Chem Lett ; 9(5): 759-64, 1999 Mar 08.

Article en En | MEDLINE | ID: mdl-10201843

RESUMEN

A novel series of benzo[b]thiophene diamine thrombin inhibitors with a conformationally restricted C3-side chain 3 was investigated. The constrained C3-side chain by a cyclohexyl ring contributed to not only an additive but also a synergistic effect on the thrombin inhibitory activity. The SAR studies resulted in the discovery of a potent thrombin inhibitor 27 that was over 750-fold more potent than the initial lead compound 1.

Asunto(s)

Tiofenos/química; Trombina/antagonistas & inhibidores; Relación Estructura-Actividad; Tiofenos/farmacología

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiofenos / Trombina Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 1999 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido

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