426834-30-2Relevant academic research and scientific papers
SAR studies of 3-cyclopropanecarbonyloxy-2-cyclohexen-1-one as inhibitors of 4-hydroxyphenylpyruvate dioxygenase
Lin, Yung-Lung,Wu, Chung-Shieh,Lin, Shean-Woei,Huang, Jian-Lin,Sun, Yang-Sheng,Yang, Ding-Yah
, p. 685 - 690 (2002)
Various 3-cyclopropanecarbonyloxy-2-cyclohexen-1-one 1 derivatives have been synthesized and tested as inhibitors of 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) from pig liver. The inhibition results indicated that well-positioned dicarbonyl groups as well as the cyclopropyl group of 1 were essential for potent inhibition. Substitution at the 2-position of the ring system has a significant effect on inhibitor potency, while the 5-position can undergo substantial variations and retain inhibitor potency. In the compounds examined, 2-chloro substituted 12 is the best inhibitor of all with IC50 of 15 nM, the rest of the synthesized analogues were less potent inhibitors than the parent compound.
