85293-40-9Relevant articles and documents
Design, synthesis, and bioevaluation of a novel class of (E)-4-oxo-crotonamide derivatives as potent antituberculosis agents
Ren, Jinfeng,Xu, Jian,Zhang, Guoning,Xu, Changliang,Zhao, LiLi,You, XueFu,Wang, Yucheng,Lu, Yu,Yu, Liyan,Wang, Juxian
, p. 539 - 543 (2019/01/09)
A series of novel (E)-4-oxo-2-crotonamide derivatives were designed and synthesized to find potent antituberculosis agents. All the target compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis H37Rv(MTB). Results reveal that 4-phenyl moiety at part A and short methyl group at part C were found to be favorable. Most of the derivatives displayed promising activity against MTB with MIC ranging from 0.125 to 4 μg/mL. Especially, compound IIIa16 was found to have the best activity with MIC of 0.125 μg/mL against MTB and with MIC in the range of 0.05–0.48 μg/mL against drug-resistant clinical MTB isolates.
Gastro-protecting activity
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, (2008/06/13)
Diseases and ailments accompanied by gastric and gastroduodenal lesions treated by administering a compound of the formula (I) STR1 in which R represents hydrogen or alkyl containing 1 to 5 carbon atoms and R1 and R2, identical or different, both represent alkoxy containing 1 to 3 carbon atoms, or both represent halogen, or R1 represents hydrogen and R2 represents halogen, nitro or trifluoromethyl, or R1 and R2 form a methylenedioxy group at adjacent carbon atoms, as well as pharmaceutically acceptable salts thereof, particularly alkali metal, alkaline earth metal, or amine salts of said acid.