The human immunodeficiency virus type 1 (HIV‐1) is the major etiological agent responsible for the acquired immunodeficiency syndrome (AIDS), which is a serious infectious disease and remains one of the most prevalent problems at present. Currently, combined antiretroviral therapy is the primary modality for the treatment and management of HIV/AIDS, but the long‐term use can result in major drawbacks such as the development of multidrug‐resistant viruses and multiple side effects. 1,2,3‐Triazole is the common framework in the development of new drugs, and its derivatives have the potential to inhibit various HIV‐1 enzymes such as reverse transcriptase, integrase, and protease, consequently possessing a potential anti‐HIV‐1 activity. This review covers the recent advances regarding the 1,2,3‐triazole hybrids with potential anti‐HIV‐1 activity; it focuses on the chemical structures, structure–activity relationship, and mechanisms of action, covering articles published from 2010 to 2020.
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