Heterocycle fused cyclohexylglycine derivatives as novel dipeptidyl peptidase-IV inhibitors

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 de...

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Bibliographic Details
Published inHeterocycles Vol. 62; pp. 203 - 206
Main Authors Mastracchio, A, Parmee, ER, Leiting, B, Marsilio, F, Patel, R, Thornberry, NA, Weber, AE, Edmondson, SD
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier 01.01.2004
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
dipeptidyl peptidase IV
Hantzsch synthesis
indole or thiazole fused cyclohexyl glycine
Fisher indole synthesis
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Summary: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).
ISSN:0385-5414
DOI:10.3987/COM-03-S(P)50