Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 15, Issue 20, Pages 6535-6548Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.07.010
Keywords
obesity; PTP1B inhibitor; protein tyrosine phosphatase; diet-induced obesity; salicylic acid; disalicylic acid; methylenedisalicylic acid
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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. (c) 2007 Elsevier Ltd. All rights reserved.
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