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Most Intriguing Documents 4Q07-Chemistry and Related Science

Following is one of the journal documents most requested by researchers using CAS online services.

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CAS indexed 71 chemical substances from this document. CAS subject entries for this document include: Adipose tissue; Anticholesteremic agents; Antiobesity agents; and 10 additional concepts

CAPLUS COPYRIGHT 2008 ACS on STN

TITLE:	Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs
AUTHOR(S):	Shrestha, Suja; Bhattarai, Bharat Raj; Lee, Keun-Hyeung; Cho, Hyeongjin
CORPORATE SOURCE:	Department of Chemistry and Institute of Molecular Cell Biology, College of Natural Sciences, Inha University, Incheon, 402-751, S. Korea
SOURCE:	Bioorganic & Medicinal Chemistry (2007), 15(20), 6535-6548 CODEN: BMECEP; ISSN: 0968-0896
PUBLISHER:	Elsevier Ltd.
LANGUAGE:	English

ABSTRACT:
A series of compds. contg. one or two salicylic acid moieties were synthesized, and their efficacy to inhibit the phosphohydrolase activity of PTP1B examd. Some of the methylenedisalicylic acid derivs. were potent inhibitors of PTP1B. Of those derivs., 3c exhibited about a 14-fold selectivity against TC-PTP, and this compd. was tested in a mouse model for its efficacy to prevent diet-induced obesity. It effectively suppressed the increases in body wt. and adipose mass, without any noticeable toxic effect. The compd. also prevented increases in the plasma triglyceride, cholesterol, and nonesterified fatty acid concns.; thus, expanding its therapeutic potential to other related metabolic diseases, such as hyperlipidemia and hypercholesterolemia.