Novel Oxindoles as Potent Anti-HIV Agents

摘要

Non-nucleoside reverse transcriptase inhibitors (NNRTI's) are a major component of the current therapy for AIDS. However, in recent years, significant resistance has been generated against the marketed NNRTI's (nevirapine, delavirdine and efavirenz) due to viral mutations. New NNRTI's are needed to overcome the increasing resistance. We have discovered a novel series of oxindoles that exhibit single digit nanomolar potency against WT HIV and drug-resistant mutants. The synthesis and structure activity relationship (SAR) of this novel series of NNRTI's will be discussed.