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Bioorg Med Chem Lett
; 20(3): 1109-13, 2010 Feb 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-20031405
RESUMEN
Design, synthesis, and SAR are described for a class of DPP-IV inhibitors based on aminobenzo[a]quinolizines with non-aromatic substituents in the S1 specificity pocket. One representative thereof, carmegliptin (8p), was chosen for clinical development. Its X-ray structure in complex with the enzyme and early efficacy data in animal models of type 2 diabetes are also presented.