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ID: ALA1139622
Journal: Bioorg Med Chem Lett
Title: Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.
Authors: 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.
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.
CiteXplore: 15908206