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Synthesis of novel tetrazole tetrahydrobenzo[b]thiophene via Ugi-MCR: As new antileishmanial prototype
Journal of Saudi Chemical Society ( IF 5.6 ) Pub Date : 2021-06-29 , DOI: 10.1016/j.jscs.2021.101295
Sultan Pathan , Girdhar Pal Singh

A new series of tetrazole series of tetrazole tetrahydrobenzo[b]thiophene (10a-l) were synthesized and evaluated as antileishmanial activity and cytotoxicity of in vitro. The results showed that compound 10k has been most potent in vitro studies, which is threefold significant active with IC50 values of 2.48 μM and it is highly selective than that of miltifosine. Compound 10k antipromastigote activity is 100 ± 0 which is comparative to miltifosine. Tetrazole tetrahydrobenzo[b]thiophene has synthesized by Gewald synthesis followed by Ugi multicomponent reaction in presence of aldehyde, isocyanide and azide. The yield is quantitative. The identity of newly synthesized tetrazole compounds has been achieved via spectroscopic analysis like 1H NMR, 13C NMR, and mass spectra.



中文翻译:

通过 Ugi-MCR 合成新型四唑四氢苯并 [b] 噻吩:作为新的抗利什曼原虫

合成了新系列的四唑四氢苯并[b]噻吩(10a-l),并评估了体外抗利什曼病活性和细胞毒性。结果表明,化合物 10k 是最有效的体外研究,其具有三倍的显着活性,IC50 值为 2.48 μM,并且比米替福新具有高度选择性。与米替福新相比,化合物 10k 抗前鞭毛体的活性为 100 ± 0。四唑四氢苯并[b]噻吩通过Gewald合成法合成,然后在醛、异氰化物和叠氮化物存在下进行Ugi多组分反应。产量是定量的。新合成的四唑化合物已通过光谱分析如1 H NMR、13C NMR和质谱。

更新日期:2021-07-07
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