Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors.
A new series of pyrazolidine derivatives was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 9i was the most active in this series, exhibited IC50 value of 1.56 microM and ED50 value of 80 mg/kg (in vivo DP-IV inhibition; po).
Ahn
Jin Hee
JH
Medicinal Science Division, Korea Research Institute of Chemical Technology, Taejon 305-600, Republic of Korea. jhahn@krict.re.kr
Kim
Jin Ah
JA
Kim
Hye-Min
HM
Kwon
Hyuk-Man
HM
Huh
Sun-Chul
SC
Rhee
Sang Dal
SD
Kim
Kwang Rok
KR
Yang
Sung-Don
SD
Park
Sung-Dae
SD
Lee
Jae Mok
JM
Kim
Sung Soo
SS
Cheon
Hyae Gyeong
HG
D018819:Dipeptidyl Peptidase 4 / Q000187:drug effects*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D011720:Pyrazoles; D018819:Dipeptidyl Peptidase 4