Abstract

Human immunodeficiency virus is responsible for acquired immunodeficiency syndrome (AIDS), an infectious disease that consists a serious concern worldwide for more than three decades. By the end of 2013 UNAIDS estimated that there were 35 million (range 33.2–37.2 million) adults and children living with HIV/AIDS worldwide. Despite the introduction of highly active antiretroviral therapy (HAART), the need for new anti-HIV agents is extremely high because the existing medicines do not provide the complete curation and exhibit serious side effects, and their application leads to the appearance of resistant strains. This chapter explores the medicinal chemistry efforts that gave rise to currently launched drugs as well as investigational anti-HIV agents. Currently used and studied molecular targets of antiretrovirals and the main classes of HIV-1 inhibitors are presented. Among the future prospects, we discuss the efforts directed to overcome the latent HIV infection, utilization of natural products as potential anti-HIV agents, recent trends on development of biologics as potential anti-HIV medicines, and application of computer-aided methods in the discovery of new anti-HIV drugs.

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