Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors

被引：77

作者：

Lau, CK

Bayly, CI

Gauthier, JY

Li, CS

Therien, M

Asante-Appiah, E

Cromlish, W

Boie, Y

Forghani, F

Desmarais, S

Wang, QP

Skorey, K

Waddleton, D

Payette, P

Ramachandran, C

Kennedy, BP

Scapin, G

机构：

[1] Merck Frosst Ctr Therapeut Res, Dept Med Chem, Pointe Claire, PQ H9R 4P8, Canada

[2] Merck Frosst Ctr Therapeut Res, Dept Biochem & Mol Biol, Pointe Claire, PQ H9R 4P8, Canada

[3] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 04期

关键词：

D O I：

10.1016/j.bmcl.2003.11.076

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of benzotriazole phenyldifluoromethylphosphonic acids were found to be potent PTP-1B inhibitors. Molecular modeling on the X-ray crystal structure of the lead structure led to the design of potent PTP-1B inhibitors that show moderate selectivity against TC-PTP, a very closely related protein tyrosine phosphatase. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：1043 / 1048

页数：6

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