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Current Developments in the Synthesis and Biological Activity of HIV-1 Double-Drug Inhibitors

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A combination of different HIV inhibitors into a single molecular entity is a strategy that is growing in popularity in HIVchemotherapy research. The high levels of resistance elicited by both nucleoside and non-nucleoside reverse transcriptase inhibitors has prompted the design of double-drugs combining these two entities with the aim of addressing the emergence of resistance. The strategy involves combining two different inhibitors into a single chemical entity via a linker, with the aim of improving the physicochemical characteristics of the individual compounds. Linkers may be sub-divided into cleavable and non-cleavable. While the former result in regeneration of the parent drugs of the double-drug once in the cell cytoplasm, the latter type is designed to allow the double-drug to target two active sites in a simultaneous or bifunctional fashion, which are located in close proximity. The linkers have been attached at the C-5', C-5 or N-3 positions of the nucleoside, and in some of the substrates synthesized, a synergistic anti-HIV activity has been observed. This review focuses on the design and synthesis of anti-HIV double-drugs reported to date.
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Keywords: Anti-HIV; Bifunctional drugs; Chemokine Receptor; Combination therapy; Double-drug; NNRTI; NRTI; Protease; Reverse Transcriptase

Document Type: Research Article

Affiliations: Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

Publication date: 01 May 2007

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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