Next Article in Journal
Ent-Abietanoids Isolated from Isodon serra
Next Article in Special Issue
Design of Drug Delivery Systems Containing Artemisinin and Its Derivatives
Previous Article in Journal
Adsorptive Desulfurization of Model Gasoline by Using Different Zn Sources Exchanged NaY Zeolites
Previous Article in Special Issue
Synthetic Approaches to Mono- and Bicyclic Perortho-Esters with a Central 1,2,4-Trioxane Ring as the Privileged Lead Structure in Antimalarial and Antitumor-Active Peroxides and Clarification of the Peroxide Relevance
Article Menu
Issue 2 (February) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(2), 303;

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

Molecular Design and Synthesis, Department of Chemistry, KU Leuven, Celestijnenlaan 200F, 3001 Leuven, Belgium
Department of Plant Biotechnology, Atta-Ur-Rahman School of Applied Biosciences (ASAB), National University of Sciences and Technology (NUST), H-12 Islamabad, Pakistan
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)
Full-Text   |   PDF [988 KB, uploaded 17 February 2017]   |  


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

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary material


Share & Cite This Article

MDPI and ACS Style

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top