Recent Advances in DAPYs and Related Analogues as HIV-1 NNRTIs
In this review, we first present a brief historical account of the medicinal chemistry of the DAPY NNRTIs, then focus on the extensive structural modifications, SAR studies, and binding mode analysis based on crystallographic and molecular modeling. Other structural related NNRTI scaffolds will also be reviewed.
Keywords: Acquired immune deficiency syndrome (AIDS); DAPY; DAPY NNRTIS; Free energy perturbation; HIV-1; NNRTIs; TMC125; TMC278; X-ray crystallographic; aryl groups; computa-tional chemistry; crystallography; cytotoxicity; deaths; di-arylpyrimidine; drug design; drug-resistance; highly ac-tive antiretroviral therapy (HAART); imidoyl thiourea; ligand binding; nucleoside re-verse transcriptase inhibitors (NRTIs); pandemic diseases; pharmacokinetic; potency; pyrazinones; torsional flexibility; vaccine; vaginal HIV microbicide
Document Type: Research Article
Publication date: 2011-01-01
- 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.