Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses

Autor:	Vandna Munshi, Joe P. Vacca, Sinoeun Touch, Gregory Moyer, Jessica A. Flynn, Peter J. Felock, Dai-Shi Su, Theresa M. Williams, Deanne Rudd, Neville J. Anthony, Meiquing Lu, Michael W. Miller, Carolyn Bahnck, Rebecca Perlow-Poehnelt, Daniel J. DiStefano, John Jin Lim, Rosa I. Sanchez, Bang-Lin Wan, Kenneth D. Anderson, Elizabeth Tinney, Ming-Tain Lai, Mary Beth Young, Yuexia Liang
Rok vydání:	2009
Předmět:	education Ether Nucleoside Reverse Transcriptase Inhibitor Cell Line chemistry.chemical_compound Structure-Activity Relationship Dogs Drug Discovery Pyrazolopyridine medicine Potency Structure–activity relationship Animals Humans Reverse-transcriptase inhibitor Chemistry Nucleosides Nucleotidyltransferase Macaca mulatta humanities Reverse transcriptase HIV Reverse Transcriptase Rats Biochemistry Mutation HIV-1 Molecular Medicine Reverse Transcriptase Inhibitors medicine.drug Ethers
Zdroj:	Journal of medicinal chemistry. 52(22)
ISSN:	1520-4804
Popis:	Biaryl ethers were recently reported as potent NNRTIs. Herein we disclose a detailed SAR study that led to the biaryl ether 6. This compound possessed excellent potency against WT RT and key clinically observed RT mutants and had an excellent pharmacokinetic profile in rats, dogs, and rhesus macaques. The compound also exhibited a clean safety profile in preclinical safety studies.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2e35dad9216b03d007b82fd31ea973a https://pubmed.ncbi.nlm.nih.gov/19883100 Zobrazit plný text záznamu