| Title : Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors - Edmondson_2005_Bioorg.Med.Chem.Lett_15_3048 |
| Author(s) : Edmondson SD , Mastracchio A , Duffy JL , Eiermann GJ , He H , Ita I , Leiting B , Leone JF , Lyons KA , Makarewicz AM , Patel RA , Petrov A , Wu JK , Thornberry NA , Weber AE |
| Ref : Bioorganic & Medicinal Chemistry Lett , 15 :3048 , 2005 |
|
Abstract :
anti-Substituted biaryl beta-methylphenylalanine derived amides have been shown to be potent DPP-IV inhibitors that suffer from suboptimal selectivity and pharmacokinetics. This letter describes the substitution of the beta-methyl substituent with beta-polar substituents, culminating in the discovery of a beta-dimethylamide substituted phenylalanine derivative with an excellent potency, selectivity, and pharmacokinetic profile. |
| PubMedSearch : Edmondson_2005_Bioorg.Med.Chem.Lett_15_3048 |
| PubMedID: 15908206 |
Edmondson SD, Mastracchio A, Duffy JL, Eiermann GJ, He H, Ita I, Leiting B, Leone JF, Lyons KA, Makarewicz AM, Patel RA, Petrov A, Wu JK, Thornberry NA, Weber AE (2005)
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett
15 :3048
Edmondson SD, Mastracchio A, Duffy JL, Eiermann GJ, He H, Ita I, Leiting B, Leone JF, Lyons KA, Makarewicz AM, Patel RA, Petrov A, Wu JK, Thornberry NA, Weber AE (2005)
Bioorganic & Medicinal Chemistry Lett
15 :3048