Application of the Triazolization Reaction to Afford Dihydroartemisinin Derivatives with Anti-HIV Activity

作者：Jana Sampad; Iram Shabina; Thomas Joice; Hayat Muhammad Qasim; Pannecouque Christophe^*; Dehaen Wim^*

来源：Molecules, 2017, 22(2): 303.

DOI：10.3390/molecules22020303

• triazole
• artemisinin
• triazolization
• organocatalytic
• multicomponent reaction

Artemisinin and synthetic derivatives of dihydroartemisinin are known to possess various biological activities. Post-functionalization of dihydroartemisinin with triazole heterocycles has been proven to lead to enhanced therapeutic potential. By using our newly developed triazolization strategy, a library of unexplored fused and 1,5-disubstituted 1,2,3-triazole derivatives of dihydroartemisinin were synthesized in a single step. All these newly synthesized compounds were characterized and evaluated for their anti-HIV (Human Immunodeficiency Virus) potential in MT-4 cells. Interestingly; three of the synthesized triazole derivatives of dihydroartemisinin showed activities with half maximal inhibitory concentration (IC50) values ranging from 1.34 to 2.65 mu M.

• 出版日期2017-2
• 单位河北医科大学