4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors

Autor:	Soo S. Ko, Susan Jeffrey, Sharon Diamond, Carolyn A. Weigelt, Susan Erickson-Viitanen, James D. Rodgers, Beverly C. Cordova, Dennis R. Chidester, Anthony J. Cocuzza, Ronald M. Klabe, Lee T. Bacheler
Rok vydání:	2001
Předmět:	Cyclopropanes Efavirenz Stereochemistry Clinical Biochemistry Pharmaceutical Science Pharmacology Biochemistry Chemical synthesis Virus chemistry.chemical_compound Structure-Activity Relationship Drug Discovery Oxazines Structure–activity relationship Animals Humans Molecular Biology Quinazolinones chemistry.chemical_classification biology Chemistry Organic Chemistry virus diseases Nucleotidyltransferase Macaca mulatta Reverse transcriptase HIV Reverse Transcriptase Benzoxazines Enzyme Enzyme inhibitor Alkynes biology.protein Quinazolines Molecular Medicine Reverse Transcriptase Inhibitors Protein Binding
Zdroj:	Bioorganicmedicinal chemistry letters. 11(11)
ISSN:	0960-894X
Popis:	A series of 4,1-benzoxazepinone analogues of efavirenz (Sustiva) as potent NNRTIs has been discovered. The cis-3-alkylbenzoxazepinones are more potent then the trans isomers and can be synthesized preferentially by a novel stereoselective cyclization. The best compounds are potent orally bioavailable inhibitors of both wild-type HIV-1 and its clinically relevant K103N mutant virus, but are highly protein-bound in human plasma.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::481bae31c062846d1d9cb99aaec62b20 https://pubmed.ncbi.nlm.nih.gov/11378361 Zobrazit plný text záznamu Full Text from ScienceDirect