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Functional Roles of Azoles Motif in Anti-HIV Agents

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Currently, there has been considerable interest in the discovery of original molecules with broad-spectrum anti- HIV activity and favourable pharmacokinetic profiles, to be used as an alternative to the approved anti-HIV/AIDS drugs, should they fail as therapeutics. Five-membered azole heterocycles represent an important class of lead structures for novel anti-HIV drug development. They can serve as versatile building blocks to introduce different new functional groups, (i) as scaffolds to anchor these groups into the optimal space for interactions with the target, (ii) as basic pharmacophore elements to make hydrogen bonds or hydrophobic interaction for facilitating the spatial filling at the binding site, (iii) as ester surrogates to improve metabolic stability, or (iv) as pharmacophoric motif of metal coordination to coordinate metal ions (i.e. magnesium) within the active site of target (i.e. integrase). This article will summarize recent progress in the development of some azoles derivatives that inhibit the replication of HIV-1 and will illustrate the possible functional role(s) of the azole motif in the search for new anti-HIV drugs.

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Keywords: AIDS; Aromatic; DNA; HIV; Heterocycle; Metal Coordination; Peptide Bond Isostere; Ritonavir; X-ray crystallography; acquired immune deficiency syndrome (AIDS); amino acid; antagonist; antiretroviral drugs; aromatic side chains; azole rings; azole-based antiviral agents; azoles; benzene; bioavailability; biochemistry; bioisosteres; bioisosters; biological activity; blood plasma; carbonyl group; chemogenomics; chemoinformatics; drug-resistant viruses; efficacy; ester; heteroaromatic carboxylic acid; heterocycle; heterocyclic thiazolyl; hydrogen bonds; long-term drug; morbidity; mortality; mutations; non-nucleoside; novel orally; optimization; orientation; orthogonal; oxadiazole; pharmacokinetic; pharmacophore; physico-chemical properties; potency; pyrazole; strains; thiadiazole; thioesters

Document Type: Research Article

Publication date: 2011-01-01

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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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