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

Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs. Research Abstract Details 

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

Suja Shrestha,Bharat Raj Bhattarai,Keun-Hyeung Lee,Hyeongjin Cho,Suja Shrestha,Bharat Raj Bhattarai,Keun-Hyeung Lee,Hyeongjin Cho,

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 increases in body weight and adipose mass, without any noticeable toxic effect. The compound also prevented increases in the plasma triglyceride, cholesterol, and nonesterified fatty acid concentrations; thus, expanding its therapeutic potential to other related metabolic diseases, such as hyperlipidemia and hypercholesterolemia.

Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs. Publishing Authors By Initials

S Shrestha,BR Bhattarai,KH Lee,H Cho,S Shrestha,BR Bhattarai,KH Lee,H Cho,

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

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Bioorganic & medicinal chemistry

VOLUME: 15

Page Numbers: 6535-48

Journal Abbreviation: Bioorg. Med. Chem.

ISSN: 0968-0896

DAY: 26

MONTH: 07

YEAR: 2007

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

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LANGUAGE: eng

NlmUniqueID: 9413298

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Grant and Affiliation Information for Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs.

AFFILIATION: Department of Chemistry and Institute of Molecular Cell Biology, College of Natural Sciences, Inha University, Incheon 402-751, Republic of Korea.

Country: England

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MEDLINETA: Bioorg Med Chem

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