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2004
Pyrazole derivatives
R 0180
Synthesis and DP-IV Inhibition of Cyano-Pyrazoline Derivatives as Potent AntidiAgents. — To increase the in vivo stability of a recently reported cyano-pyra52- 105 abetic
zoline based dipeptidyl peptidase IV inhibitor, the amino acid part of this compound is
modified by synthesizing cyano-pyrazoline derivatives with a secondary amine at P-2
site. Racemic and chiral cyano-pyrazoline derivatives are prepared. N-Alkyl substituents at P-2 show moderate in vitro activities whereas heteroaryls (VII) show better
activities. Compound (VIIa) displays good in vivo DP-IV inhibition. The chiral version
(S)-(VIIa), is found to be 2-fold more potent. — (AHN*, J. H.; KIM, H.-M.; JUNG, S.
H.; KANG, S. K.; KIM, K. R.; RHEE, S. D.; YANG, S.-D.; CHEON, H. G.; KIM, S. S.;
Bioorg. Med. Chem. Lett. 14 (2004) 17, 4461-4465; Med. Sci. Div., Korea Res. Inst.
Chem. Technol., Taejon 305-600, S. Korea; Eng.) — H. Hoennerscheid
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