3,3a-Dihydropyrano[4,3,2- de ]quinazolin-2(1 H )-ones are potent non-nucleoside reverse transcriptase inhibitors

Autor:	Jay A. Markwalder, Senliang Pan, Jeffrey W. Corbett, Beverly C. Cordova, James D. Rodgers, Sena Garber, Susan Erickson-Viitanen, Ronald M. Klabe
Rok vydání:	2001
Předmět:	Models Molecular Efavirenz Stereochemistry Clinical Biochemistry Mutant Drug Resistance Pharmaceutical Science Heterocyclic Compounds 2-Ring Biochemistry Virus Nucleoside Reverse Transcriptase Inhibitor Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Combinatorial Chemistry Techniques Humans Point Mutation Molecular Biology Pyrans chemistry.chemical_classification Binding Sites biology Organic Chemistry Nucleotidyltransferase HIV Reverse Transcriptase Reverse transcriptase Enzyme chemistry Enzyme inhibitor Quinazolines biology.protein Reverse Transcriptase Inhibitors Molecular Medicine Heterocyclic Compounds 3-Ring
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 11:211-214
ISSN:	0960-894X
Popis:	A series of unique 3,3a-dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones and a 2a,5-dihydro-2H-thieno[4,3,2-de]quinazoline-4(3H)-thione were found to be HIV-1 non-nucleoside reverse transcriptase inhibitors. One of these compounds, as the racemate, possessed an IC90=4.6 nM against wild-type virus in a whole cell antiviral assay and had an IC90=76 and 897 nM against the clinically significant K103N and K103N/L100I mutant viruses, respectively.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::269c5f147dd18301128eb016bde7ac18 https://doi.org/10.1016/s0960-894x(00)00624-7 Zobrazit plný text záznamu Full Text from ScienceDirect