Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors

…, Y Hu, T Nomanbhoy, S Alemayehu, SR Fuller…

文献索引：Shreder, Kevin R.; Wong, Melissa S.; Corral, Sergio; Yu, Zhizhou; Winn, David T.; Wu, Min; Hu, Yi; Nomanbhoy, Tyzoon; Alemayehu, Senaiet; Fuller, Stacy R.; Rosenblum, Jonathan S.; Kozarich, John W. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 19 p. 4256 - 4260

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被引用次数: 15

摘要

Dipeptide-based inhibitors with C-substituted (alkyl or aminoalkyl) α-amino acids in the P2 position and boro-norleucine (boro-Nle) in the P1 position were synthesized. Relative to boro-proline, boro-Nle as a P1 residue was shown able to significantly dial out DPP4, FAP, DPP8, and DPP9 activity. Dab-boro-Nle (4g) proved to be the most selective and potent DPP7 inhibitor with a DPP7 IC50 value of 480pM.