Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp3 values and favorable drug-like properties
Xiangyi Jiang, Boshi Huang, Fisayo A. Olotu, Jing Li, Dongwei Kang, Zhao Wang, Erik De Clercq, Mahmoud E. S. Soliman, Christophe Pannecouque, Xinyong Liu, Peng Zhan
Topics & Concepts
EtravirineChemistryReverse transcriptaseReverse-transcriptase inhibitorNucleoside Reverse Transcriptase InhibitorEC50StereochemistryDrug discoveryDocking (animal)CytotoxicityNucleosideRilpivirineHuman immunodeficiency virus (HIV)VirologyIn vitroBiochemistryViral loadRNABiologyAntiretroviral therapyGeneNursingMedicineHIV/AIDS drug development and treatmentHIV Research and TreatmentDNA and Nucleic Acid Chemistry