Potent and selective proline derived dipeptidyl peptidase IV inhibitors

In-house screening of the Merck sample collection identified proline derived homophenylalanine 3 as a DPP-IV inhibitor with modest potency (DPP-IV IC50=1.9μM). Optimization of 3 led to compound 37, which is among the most potent and selective DPP-IV inhibitors discovered to date. In-house screening...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-10, Vol.14 (20), p.5151-5155
Hauptverfasser:	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.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Biological and medical sciences Biological Availability Dipeptidyl Peptidase 4 - metabolism Dipeptidyl peptidase IV Humans In Vitro Techniques Medical sciences Miscellaneous Pharmacology. Drug treatments Proline - analogs & derivatives Proline - chemical synthesis Proline - chemistry Proline - pharmacology Proline amide Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Rats Selective Structure-Activity Relationship Thiazolidine Type 2 diabetes
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Beschreibung
Zusammenfassung:	In-house screening of the Merck sample collection identified proline derived homophenylalanine 3 as a DPP-IV inhibitor with modest potency (DPP-IV IC50=1.9μM). Optimization of 3 led to compound 37, which is among the most potent and selective DPP-IV inhibitors discovered to date. In-house screening of the Merck sample collection identified proline derived homophenylalanine 3 as a DPP-IV inhibitor with modest potency (DPP-IV IC50=1.9μM). Optimization of 3 led to compound 37, which is among the most potent and selective DPP-IV inhibitors discovered to date.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.07.056