摘要
A series of novel tetrazole containing 1,2,3-thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by melting points, IR, 1H NMR, and HRMS （ESI）. Preliminary bioassay indicated that most target compounds exhibited very good direct anti-TMV activity at 100 μg/mL, which was equal to or higher than that of ribavirin. Among them, compounds 4b, 4c and 4i also showed equivalent protection effect to ribavirin in vivo at 100 μg/mL.
A series of novel tetrazole containing 1,2,3-thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by melting points, IR, 1H NMR, and HRMS （ESI）. Preliminary bioassay indicated that most target compounds exhibited very good direct anti-TMV activity at 100 μg/mL, which was equal to or higher than that of ribavirin. Among them, compounds 4b, 4c and 4i also showed equivalent protection effect to ribavirin in vivo at 100 μg/mL.
基金
funded in part by the NSF of Tianjin (No. 10JCZDJC17500)
the National Key Project for Basic Research (No. 2010CB126105)
National Key Technology Research and Development Program (No. 2011BAE06B02)
the Foundation of Achievements Transformation and Application of Tianjin Agricultural Science and Technology (No. 201002250)
Tianjin Key Technology Research and Development Program (No. 11ZCGYNC00100)
The Commonweal Specialized Research Fund of China Agriculture (Nos. nyhyzx3-21, 201103016 and 201003029)
