2-(1-苯基/取代苯基-3-甲基-5-氯-1H-4-吡唑基)-3-芳酰胺-4-噻唑啉酮的合成及生物活性

Synthesis and Biological Activities of 2-(1-Aryl-3-methyl-5-chloro- 1H-pyrazol-4-yl)-3-(1-aroylamino)-4-thiazolidinones

利用1-芳基-3-甲基-5-氯-1H-4-吡唑醛(2)分别与取代苯甲酰肼反应,进一步与巯基乙酸关环,合成了11个新的2-(1-芳基-3-甲基-5-氯-1H-4-吡唑基)-3-芳酰胺-4-噻唑啉酮类化合物3a～3k,并利用元素分析,IR,HNMR和X-ray晶1体衍射确定了其结构.初步生物活性表明:3e具有杀菌活性,3e和3k具有除草活性.

The reactions of 1-aryl-3-methyl-5-chloro-1H-4-pyrazolylformaldehydes (2) with aroylhydrazines and followed by the addition of mercaptoacetic acid, eleven new compounds 2-(1-aryl-3-methyl-5chloro-1H-pyrazol-4-yl)-3-(1-aroylamino)-4-thiazolidinones 3asimilar to3k have been synthesized. Their structures were characterized by elemental analysis, IR and H-1 NMR spectra, and one of them 3d by X-ray diffraction study. The preliminary bioassay tests showed that compound 3e possessed moderate fungicidal activity and 3e and 3k only exhibited certain herbicidal activity.