title: Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents.
abstract: A new series of cyano-pyrazoline derivatives with secondary amine at P-2 site was synthesized through achiral and chiral synthetic methods and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 5i revealed good in vivo efficacy (ED50: 4.1 mg/kg; in vivo DP-IV inhibition). Also chiral derivative (11b) having (S)-configuration of compound 5i was found to be more potent.
authors.affiliation: Medicinal Science Division, Korea Research Institute of Chemical Technology, Yusung, Taejon 305-600, South Korea. jhahn@krict.re.kr
authors.forename: Jin Hee
authors.initials: JH
authors.lastname: Ahn
authors.forename: Hye-Min
authors.initials: HM
authors.lastname: Kim
authors.forename: Sun Ho
authors.initials: SH
authors.lastname: Jung
authors.forename: Seung Kyu
authors.initials: SK
authors.lastname: Kang
authors.forename: Kwang Rok
authors.initials: KR
authors.lastname: Kim
authors.forename: Sang Dal
authors.initials: SD
authors.lastname: Rhee
authors.forename: Sung-Don
authors.initials: SD
authors.lastname: Yang
authors.forename: Hyae Gyeong
authors.initials: HG
authors.lastname: Cheon
authors.forename: Sung Soo
authors.initials: SS
authors.lastname: Kim
mesh_terms: D000818:Animals; D018938:Caco-2 Cells; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D008810:Mice, Inbred C57BL; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013552:Swine
chemical_list: D007004:Hypoglycemic Agents; D011480:Protease Inhibitors; D011720:Pyrazoles; C415802:DP IV-related protease, human; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases