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Communication | Special issue | Vol 62, No. 1, 2004, pp.203-206
Published online, 14th November, 2003
DOI: 10.3987/COM-03-S(P)50
Heterocycle Fused Cyclohexylglycine Derivatives as Novel Dipeptidyl Peptidase-IV Inhibitors

Anthony Mastracchio,* Emma R. Parmee, Barbara Leiting, Frank Marsilio, Reshma Patel, Nancy A. Thornberry, Ann E. Weber, and Scott D. Edmondson

*Division of Merck & Co., Inc., Merck Research Laboratories, P.O.Box 2000, Rahway, NJ 07065, U.S.A.

Abstract

A new class of potent inhibitors of dipeptidyl peptidase IV (DP-IV) for the treatment of type II diabetes are described. Presented herein is the synthesis of indole-fused and thiazole-fused cyclohexylglycines. Pyrrolidine-derived amides of these novel heterocycles led to the discovery of thiazole derivatives (3f) and (11a), both low nanomolar inhibitors of DP-IV (IC50 = 6 nM).