Potent Non-Nitrile Dipeptidic Dipeptidyl Peptidase IV Inhibitors

Authors

Ligaya M. Simpkins, Bristol-Myers Squibb
Scott Bolton, Bristol-Myers Squibb
Zulan Pi, Bristol-Myers Squibb
James C. Sutton, Bristol-Myers Squibb
Chet Kwon, Bristol-Myers Squibb
Guohua Zhao, Bristol-Myers Squibb
David R. Magnin, Bristol-Myers Squibb
David J. Augeri, Bristol-Myers Squibb
Timur Gungor, Bristol-Myers Squibb
David Rotella, Montclair State UniversityFollow
Zhong Sun, Bristol-Myers SquibbFollow
Yajun Liu, Bristol-Myers Squibb
William S. Slusarchyk, Bristol-Myers Squibb
Jovita Marcinkeviciene, Bristol-Myers Squibb
James G. Robertson, Bristol-Myers Squibb
Aiying Wang, Bristol-Myers Squibb
Jeffrey A. Robl, Bristol-Myers Squibb
Karnail S. Atwal, Bristol-Myers Squibb
Robert L. Zahler, Bristol-Myers Squibb
Rex A. Parker, Bristol-Myers Squibb
Mark S. Kirby, Bristol-Myers Squibb
Lawrence G. Hamann, Bristol-Myers Squibb

Document Type

Article

Publication Date

12-1-2007

Abstract

The synthesis and structure-activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with β-branched natural and unnatural amino acids, particularly adamantylglycines, linked to a (2S,3R)-2,3-methanopyrrolidine based scaffold.

DOI

10.1016/j.bmcl.2007.09.090

Montclair State University Digital Commons Citation

Simpkins, Ligaya M.; Bolton, Scott; Pi, Zulan; Sutton, James C.; Kwon, Chet; Zhao, Guohua; Magnin, David R.; Augeri, David J.; Gungor, Timur; Rotella, David; Sun, Zhong; Liu, Yajun; Slusarchyk, William S.; Marcinkeviciene, Jovita; Robertson, James G.; Wang, Aiying; Robl, Jeffrey A.; Atwal, Karnail S.; Zahler, Robert L.; Parker, Rex A.; Kirby, Mark S.; and Hamann, Lawrence G., "Potent Non-Nitrile Dipeptidic Dipeptidyl Peptidase IV Inhibitors" (2007). Department of Chemistry and Biochemistry Faculty Scholarship and Creative Works. 400.
https://digitalcommons.montclair.edu/chem-biochem-facpubs/400