Bioorg Med Chem Lett. 2009 Sep 1;19(17):5021-5. Epub 2009 Jul 12.

Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor.

Gupta RC, Chhipa L, Mandhare AB, Zambad SP, Chauthaiwale V, Nadkarni SS, Dutt C.

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Medicinal Chemistry, Torrent Research Centre, Torrent Pharmaceuticals Ltd., Gandhinagar, Gujarat, India. rameshgupta@torrentpharma.com

Abstract

A novel class of N-substituted 4-hydrazino piperidine derivatives were designed, synthesized and evaluated for DPP IV inhibition. The SAR studies on the N-substituted piperidine led to the discovery of compound 22e as a potent DPP IV inhibitor (IC(50) 88nM), which is highly selective over other peptidases. In vivo efficacy indicates that compound 22e stimulates insulin release in response to glucose load and improves glucose tolerance in n5-STZ and Zucker Diabetic Fatty (ZDF) rats.

PMID:: 19643608; [PubMed - indexed for MEDLINE]

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