Synthesis of a novel series of DPPIV inhibitors with 1,2,4- and 1,3,4-oxadiazolyl ketone derivatives and its structure-activity relationships are discussed. Compound 18h showed good inhibitory activity against DPPIV and favorable pharmacokinetic properties. In vivo pharmacodynamic efficacy and co-crystal structure of compound 18h with DPPIV is also described.
Koo KD, Kim MJ, Kim S, Kim KH, Hong SY, Hur GC, Yim HJ, Kim GT, Han HO, Kwon OH, Kwon TS, Koh JS, Lee CS (2007) Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones Bioorganic & Medicinal Chemistry Lett17: 4167-72
Koo KD, Kim MJ, Kim S, Kim KH, Hong SY, Hur GC, Yim HJ, Kim GT, Han HO, Kwon OH, Kwon TS, Koh JS, Lee CS (2007) Bioorganic & Medicinal Chemistry Lett17: 4167-72