Synthesis of New Thiadiazole-2-Oxides as Potential Antischistosomal Agents

被引：0

作者：

Zhou, Ying ^{[1
]}

Fan, Wen-Hua ^{[2
]}

Song, Li-Jun ^{[3
]}

Yu, Chuan-Xin ^{[3
]}

Feng, Bainian ^{[1
,2
]}

机构：

[1] Jiangnan Univ, Sch Pharmaceut Sci, Wuxi 214122, Jiangsu, Peoples R China

[2] Jiangshu Alpha Biopharmaceut Inc, Wuxi 214122, Jiangsu, Peoples R China

[3] Jiangsu Inst Parasit Dis, Key Lab Technol Dis Prevent & Control, Wuxi 214064, Jiangsu, Peoples R China

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2022年 / 55卷 / 10期

关键词：

antischistosomal agents; thiadiazole; 2-oxides; Schistosoma japonicum; SCHISTOSOMIASIS;

D O I：

10.1007/s11094-021-02533-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Schistosomiasis is a chronic infectious disease that affects millions of people worldwide, of which chemotherapy with praziquantel as the only available drug is the main method of control in view of the absence of effective vaccines. In this study, a series of new thiadiazole 2-oxides were synthesized as potential antischistosomal agents and evaluated in vitro for antischistosomal activity on Schistosoma japonicum adult worms. The results revealed that compound 10a (3-cyano-4-phenyl-1,2,5-thiadiazole 2-oxide) exhibited more potent worm killing activity compared to praziquantel and oxadiazole 2-oxide, which provided possible opportunity for the development of new antischistosomal drugs.

引用

页码：1028 / 1032

页数：5

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