Solid phase chemistry approach to the SAR development of a novel class of active site-directed thrombin inhibitors

被引：10

作者：

Johnson, MG

Bronson, DD

Gillespie, JE

Gifford-Moore, DS

Kalter, K

Lynch, MP

McCowan, JR

Redick, CC

Sall, DJ

Smith, GF

Foglesong, RJ

机构：

[1] Sphinx Pharmaceut, Durham, NC 27707 USA

[2] Eli Lilly & Co, Lilly Res Lab, Indianapolis, IN 46285 USA

来源：

TETRAHEDRON | 1999年 / 55卷 / 39期

关键词：

D O I：

10.1016/S0040-4020(99)00684-5

中图分类号：

O62 [有机化学];

学科分类号：

070303 [有机化学]; 081704 [应用化学];

摘要：

A solid phase chemistry approach utilizing Mitsunobu chemistry, amine functionalization. and parallel purification was used to produce a diverse library of benzothiophene analogs. These analogs were used to advance the SAR of this class of molecules and give new directions for future studies. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.

引用

页码：11641 / 11652

页数：12

共 24 条

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[2]

Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460):: Coapplication of structure-based design and rapid multiple analogue synthesis on solid support [J].