Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.

作者信息

Kurukulasuriya Ravi, Rohde Jeffrey J, Szczepankiewicz Bruce G, Basha Fatima, Lai Chunqui, Jae Hwan-Soo, Winn Martin, Stewart Kent D, Longenecker Kenton L, Lubben Thomas W, Ballaron Stephen J, Sham Hing L, von Geldern Thomas W

机构信息

Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA.

出版信息

Bioorg Med Chem Lett. 2006 Dec 15;16(24):6226-30. doi: 10.1016/j.bmcl.2006.09.024. Epub 2006 Sep 28.

DOI:10.1016/j.bmcl.2006.09.024

PMID:17010607

Abstract

A series of xanthine mimetics containing 5,5 and 5,6 heterocycle fused imidazoles were synthesized as dipeptidyl peptidase IV inhibitors. Compound 7 is potent (h-DPPIV K(i)=2nM) and exhibits excellent selectivity and no species specificity against rat and human enzymes. The X-ray structure confirms that the binding mode of 7 to rat DPPIV is similar to the parent xanthines.

摘要

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