| Title : Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones - Koo_2007_Bioorg.Med.Chem.Lett_17_4167 |
| Author(s) : 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 |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :4167 , 2007 |
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Abstract :
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. |
| PubMedSearch : Koo_2007_Bioorg.Med.Chem.Lett_17_4167 |
| PubMedID: 17544668 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | 1,3,4-oxadiazolyl-ketone-18h |
| Gene_locus | human-DPP4 |
| Structure | 2QKY |
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 Lett
17 :4167
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 Lett
17 :4167