127108-66-1Relevant articles and documents
Synthesis and biological evaluation of 4-methyl-1,2,3-thiadiazole-5-carboxaldehyde benzoyl hydrazone derivatives
Zhang, Jing-Peng,Li, Xiang-Yang,Dong, Ya-Wen,Qin, Yao-Guo,Li, Xin-Lu,Song, Bao-An,Yang, Xin-Ling
, p. 1238 - 1242 (2017)
To find new lead compounds with high biological activity, a series of novel 4-methyl-1,2,3-thiadiazole-5-carboxaldehyde benzoyl hydrazone derivatives were designed and synthesized. Their structures were confirmed by 1H NMR, 13C NMR, IR spectrum and elemental analysis. Preliminary bioassay indicated that the title compounds exhibited moderate to strong fungicidal activity against six fungi in vitro at 50?μg/mL. Moreover, some of the title compounds exhibited good curative activity against TMV in vivo at 500?μg/mL. The structure-activity relationship analysis of compounds against Valsa mali showed that compounds containing halogen at the para position on phenyl exhibited the best activity. Especially compound 8k showed broad spectrum fungicidal activities against Valsa mali, Botrytis cinerea, Pythium aphanidermatum, Rhizoctonia solani, Fusarium moniliforme and Alternaria solani with the EC50 values of 8.20, 24.42, 15.80, 40.53, 41.48, and 34.16?μg/mL, respectively.
1,2,3-thiadiazole-containing benzoyl hydrazone derivative as well as preparation method and application thereof
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Paragraph 0039; 0040; 0041; 0044; 0045, (2016/10/08)
The invention belongs to the field of organic compound synthesis and particularly relates to a 1,2,3-thiadiazole-containing benzoyl hydrazone derivative as well as a preparation method and application thereof. The structure of the compound is shown by a f
Synthesis and antiviral activity of new acrylamide derivatives containing 1,2,3-thiadiazole as inhibitors of hepatitis B virus replication
Dong, Wei-Li,Liu, Zheng-Xiao,Liu, Xing-Hai,Li, Zheng-Ming,Zhao, Wei-Guang
scheme or table, p. 1919 - 1926 (2010/06/19)
A series of new acrylamide derivatives containing 1,2,3-thiadiazole were synthesized, characterized, and evaluated for their anti-hepatitis B virus (HBV) activities in vitro. The IC50 of compounds 9b (10.4?μg/mL), 9c (3.59?μg/mL) and 17a (9.00?μg/mL) of the inhibition on the replication of HBV DNA were higher than that of the positive control lamivudine (14.8?μg/mL). Compound 9d exhibited significant activity against secretion of HBeAg (IC50?=?12.26?μg/mL).