Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase

Autor:	Ilia Korboukh, Uyen Boyle, Nanhua Yao, Huanming Chen, Esmir Gunic, Weijian Zhang, Hong Woo Kim, Matthew J. Allan, Shahul Nilar, Jean-Luc Girardet, Stanley A. Lang, Wen Xu, Cheryl Jenket, Zhijun Zhang, Zhi Hong, Yung-Hyo Koh, Robert K. Hamatake, Martha De La Rosa
Rok vydání:	2006
Předmět:	Efavirenz Stereochemistry medicine.drug_class Clinical Biochemistry Triazole Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Enzyme Inhibitors Molecular Biology Molecular Structure Reverse-transcriptase inhibitor Organic Chemistry virus diseases Nucleosides Triazoles biochemical phenomena metabolism and nutrition Nucleotidyltransferase HIV Reverse Transcriptase Reverse transcriptase chemistry HIV-1 Molecular Medicine Nucleoside medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 16:4444-4449
ISSN:	0960-894X
Popis:	A new series of 1,2,4-triazoles was synthesized and tested against several NNRTI-resistant HIV-1 isolates. Several of these compounds exhibited potent antiviral activities against efavirenz- and nevirapine-resistant viruses, containing K103N and/or Y181C mutations or Y188L mutation. Triazoles were first synthesized from commercially available substituted phenylthiosemicarbazides, then from isothiocyanates, and later by condensing the desired substituted anilines with thiosemicarbazones.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c031e880bd5c6399781472929ae5605 https://doi.org/10.1016/j.bmcl.2006.06.048 Zobrazit plný text záznamu Full Text from ScienceDirect