Triketoacid inhibitors of HIV-integrase: A new chemotype useful for probing the integrase pharmacophore
Bioorganic & Medicinal Chemistry Letters(2006)
Abstract
This study reports on the discovery of a new triketoacid-based chemotype that selectively inhibits the strand transfer reaction of HIV-integrase. SAR studies showed that the template binds to integrase in a manner similar to the diketoacid-based inhibitors. Moreover, comparison of the new chemotype to two different diketoacid templates led us to propose two aryl-binding domains in the inhibitor binding site. This information was used to design a new diketoacid template with improved activity against the enzyme.
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Key words
AIDS,HIV-integrase,Diketoacid,Triketoacid
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