Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors

The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-( S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of dipeptidyl peptidase IV (DPP IV) are reported. The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-( S)-2-cyano-pyrrolidine...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 16; no. 1; pp. 123 - 128
Main Authors:	Qiao, Lei, Baumann, Christian A., Crysler, Carl S., Ninan, Nisha S., Abad, Marta C., Spurlino, John C., DesJarlais, Renee L., Kervinen, Jukka, Neeper, Mike P., Bayoumy, Shariff S., Williams, Robyn, Deckman, Ingrid C., Dasgupta, Malini, Reed, Rolanda L., Huebert, Norman D., Tomczuk, Bruce E., Moriarty, Kevin J.
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 2006 Elsevier
Subjects:	Animals Antineoplastic Agents - pharmacology Binding Sites Biological and medical sciences Blood Glucose - metabolism Caco-2 Cells Chemistry, Pharmaceutical - methods Crystallography, X-Ray - methods Dipeptidyl Peptidase 4 - chemistry Dipeptidyl Peptidase 4 - metabolism Dipeptidyl peptidase IV Inhibitors Drug Design Drug Screening Assays, Antitumor Enzyme Inhibitors - pharmacology General and cellular metabolism. Vitamins Humans Kinetics Medical sciences Mice Models, Chemical Models, Molecular Pharmacology. Drug treatments Protease Inhibitors - pharmacology Rats SAR Structure-Activity Relationship X-ray structure SAR X-ray structure Dipeptidyl peptidase IV Inhibitors Endocrinopathy Type 2 diabetes Dipeptidyl-peptidase IV Nitrile Enzyme Enzyme inhibitor In vitro Pyrrolidine derivatives Peptidases Structure activity relation Biphenyl derivatives Hydrolases Chemical synthesis Crystalline structure
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Summary:	The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-( S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of dipeptidyl peptidase IV (DPP IV) are reported. The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-( S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of dipeptidyl peptidase IV (DPP IV) are reported.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.09.037