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Functional roles of azoles motif in anti-HIV agents.

Authors
Type
Published Article
Journal
Current medicinal chemistry
Publication Date
Volume
18
Issue
1
Pages
29–46
Identifiers
PMID: 21110816
Source
Medline

Abstract

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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