Benzophenones as inhibitors of reverse transcriptase

Abstract

HIV infection represents a serious medical problem, successfully approached ultimately by the introduction of highly active antiretroviral therapy (HAART). One class of drugs present in many HAART regimens is constituted by the non-nucleoside reverse transcriptase inhibitors (NNRTIs), with three drugs clinically available at present (nevirapine, delavirdine and efavirenz). NNRTIs successfully block HIV-1 infection by binding to the enzyme reverse transcriptase (RT), at an allosterically located, non-substrate binding site but mutations of this protein easily lead to drug-resistant viral strains. In this patent, Glaxo presents a new class of NNRTIs incorporating benzophenones and primary sulfonamide moieties, which seem to also be effective against HIV isolates resistant to the three clinically used drugs belonging to this class of pharmacological agents.

• antiviral agents
• HIV
• non-nucleoside reverse transcriptase inhibitor (NNRTI)
• reverse transcriptase inhibition
• sulfonamide