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Molecules 2017, 22(2), 303; doi:10.3390/molecules22020303

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

1
Molecular Design and Synthesis, Department of Chemistry, KU Leuven, Celestijnenlaan 200F, 3001 Leuven, Belgium
2
Department of Plant Biotechnology, Atta-Ur-Rahman School of Applied Biosciences (ASAB), National University of Sciences and Technology (NUST), H-12 Islamabad, Pakistan
3
Department of Microbiology and Immunology, Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Herestraat 49, B-3000 Leuven, Belgium
*
Authors to whom correspondence should be addressed.
Academic Editor: Svetlana B. Tsogoeva
Received: 4 January 2017 / Revised: 10 February 2017 / Accepted: 11 February 2017 / Published: 17 February 2017
(This article belongs to the Special Issue Artemisinin: Against Malaria, Cancer and Viruses)
View Full-Text   |   Download PDF [988 KB, uploaded 17 February 2017]   |  

Abstract

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 µM. View Full-Text
Keywords: triazole; artemisinin; triazolization; organocatalytic; multicomponent reaction triazole; artemisinin; triazolization; organocatalytic; multicomponent reaction
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Jana, S.; Iram, S.; Thomas, J.; Hayat, M.Q.; Pannecouque, C.; Dehaen, W. Application of the Triazolization Reaction to Afford Dihydroartemisinin Derivatives with Anti-HIV Activity. Molecules 2017, 22, 303.

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