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Potent and selective proline derived dipeptidyl peptidase IV inhibitors |
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| Authors: | Edmondson Scott D Mastracchio Anthony Beconi Maria Colwell Lawrence F Habulihaz Bahanu He Huaibing Kumar Sanjeev Leiting Barbara Lyons Kathryn A Mao Ann Marsilio Frank Patel Reshma A Wu Joseph K Zhu Lan Thornberry Nancy A Weber Ann E Parmee Emma R |
| Institution: | Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA. scott_edmondson@merck.com |
| Abstract: | In-house screening of the Merck sample collection identified proline derived homophenylalanine 3 as a DPP-IV inhibitor with modest potency (DPP-IV IC50=1.9 microM). Optimization of 3 led to compound 37, which is among the most potent and selective DPP-IV inhibitors discovered to date. |
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