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ID: ALA1141049
Journal: Bioorg Med Chem Lett
Title: Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.
Authors: Hu Y, Ma L, Wu M, Wong MS, Li B, Corral S, Yu Z, Nomanbhoy T, Alemayehu S, Fuller SR, Rosenblum JS, Rozenkrants N, Minimo LC, Ripka WC, Szardenings AK, Kozarich JW, Shreder KR.
Abstract: The structure-activity relationship of various N-alkyl Gly-boro-Pro derivatives against three dipeptidyl peptidases (DPPs) was studied. In a series of N-cycloalkyl analogs, DPP4 and fibroblast activation protein-alpha (FAP) optimally preferred N-cycloheptyl whereas DPP7 tolerated even larger cycloalkyl rings. Gly alpha-carbon derivatization of N-cyclohexyl or N-(2-adamantyl) Gly-boro-Pro resulted in a significant decrease in potency against all the three DPPs.
CiteXplore: 16085416