Mono-and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs

S Shrestha, BR Bhattarai, KH Lee, H Cho

Index: Shrestha, Suja; Bhattarai, Bharat Raj; Lee, Keun-Hyeung; Cho, Hyeongjin Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 20 p. 6535 - 6548

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Citation Number: 47

Abstract

A series of compounds containing one or two salicylic acid moieties were synthesized, and their efficacy to inhibit the phosphohydrolase activity of PTP1B examined. Some of the methylenedisalicylic acid derivatives were potent inhibitors of PTP1B. Of those derivatives, 3c exhibited about a 14-fold selectivity against TC-PTP, and this compound was tested in a mouse model for its efficacy to prevent diet-induced obesity. It effectively suppressed the ...

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