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Paper(s) concerning B2Q

1 reference(s) found.
Listing paper details in reverse chronological order.
We are grateful to Keith Bradnam for improvment of this script

Title: Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Mattei P, Boehringer M, Di Giorgio P, Fischer H, Hennig M, Huwyler J, Kocer B, Kuhn B, Loeffler BM and Sprecher U <4 more author(s)> Mattei P, Boehringer M, Di Giorgio P, Fischer H, Hennig M, Huwyler J, Kocer B, Kuhn B, Loeffler BM, Macdonald A, Narquizian R, Rauber E, Sebokova E, Sprecher U (- 4)
Ref: Bioorganic & Medicinal Chemistry Lett, 20:1109, 2010 : PubMed
Abstract


ESTHER: Mattei_2010_Bioorg.Med.Chem.Lett_20_1109
PubMedSearch: Mattei 2010 Bioorg.Med.Chem.Lett 20 1109
PubMedID: 20031405
Gene_locus related to this paper: human-DPP4
Inhibitor(s) related to this paper: Carmegliptin, B2Q

Abstract

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.