{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,10]],"date-time":"2026-09-10T15:45:10Z","timestamp":1789055110463,"version":"build-2803163510"},"reference-count":32,"publisher":"Wiley","issue":"6","license":[{"start":{"date-parts":[[2015,3,4]],"date-time":"2015-03-04T00:00:00Z","timestamp":1425427200000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["chemistry-europe.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["ChemPlusChem"],"published-print":{"date-parts":[[2015,6]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>In the continuing search for novel, biologically effective heterocyclic agents, several methods for the synthesis of 2\u2010heteroaryl\u2010[1,2,4]triazolo[1,5\u2010<jats:italic>c<\/jats:italic>]quinazoline\u20105(6\u2009<jats:italic>H<\/jats:italic>)\u2010thiones have been developed: thiolation of oxo derivatives, [5+1] cyclocondensation of [2\u2010(3\u2010heteroaryl\u2010[1,2,4]triazol\u20105\u2010yl)phenyl]amines with carbon disulfide, potassium ethyl xanthogenate, or aryl isothiocyanates, and in\u2005situ reaction of 2\u2010isothiocyanatobenzonitrile with hydrazides. A series of <jats:italic>N<\/jats:italic>\u2010<jats:italic>R<\/jats:italic>\u20102\u2010[(2\u2010heteroaryl\u2010[1,2,4]triazole\u2010[1,5\u2010<jats:italic>c<\/jats:italic>]quinazoline\u20105\u2010yl)thio]acetamides were obtained by aminolysis of the corresponding acetic acids and alkylation of potassium thiolates with <jats:italic>N<\/jats:italic>\u2010<jats:italic>R<\/jats:italic>\u20102\u2010chloroacetamides. It was established that some potassium thiolates, <jats:bold>4\u2009a<\/jats:bold>\u2013<jats:bold>4\u2009d<\/jats:bold>, <jats:bold>4\u2009h<\/jats:bold>, and <jats:bold>4\u2009i<\/jats:bold>, had high antibacterial activity against <jats:italic>Staphylococcus aureus<\/jats:italic> with a minimum inhibitory concentration of 12.5\u2005\u03bcg\u2009mL<jats:sup>\u22121<\/jats:sup> and minimum bactericidal concentration of 25\u2005\u03bcg\u2009mL<jats:sup>\u22121<\/jats:sup>, which exceeded the values for trimethoprim. In addition, {2\u2010[3\u2010(1\u2009<jats:italic>H<\/jats:italic>\u2010indole\u20102\u2010yl)\u20101\u2009<jats:italic>H<\/jats:italic>\u20101,2,4\u2010triazol\u20105\u2010yl]phenyl}amine\u2005<jats:bold>2\u2009i<\/jats:bold> was investigated in the concentration range 100\u20130.01\u2005\u03bc<jats:sc>M<\/jats:sc> at 59\u2005lines of nine cancer cell types, and showed a mean effective concentration at 3.12\u20137.03\u2005\u03bc<jats:sc>M<\/jats:sc> and cytotoxic effect at 15.56\u201367.38\u2005\u03bc<jats:sc>M<\/jats:sc>. The possible mechanisms of activity were predicted by molecular docking studies to <jats:italic>S.\u2005aureus<\/jats:italic> dihydrofolate reductase and epidermal growth factor receptor kinase.<\/jats:p>","DOI":"10.1002\/cplu.201500051","type":"journal-article","created":{"date-parts":[[2015,3,4]],"date-time":"2015-03-04T15:38:37Z","timestamp":1425483517000},"page":"980-989","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":28,"title":["2\u2010Heteroaryl\u2010[1,2,4]triazolo[1,5\u2010<i>c<\/i>]quinazoline\u20105(6\u2009H)\u2010thiones and Their S\u2010Substituted Derivatives: Synthesis, Spectroscopic Data, and Biological Activity"],"prefix":"10.1002","volume":"80","author":[{"given":"Andrii K.","family":"Bilyi","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lyudmyla M.","family":"Antypenko","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Vitalii V.","family":"Ivchuk","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Oleksandr M.","family":"Kamyshnyi","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Natalya M.","family":"Polishchuk","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sergiy I.","family":"Kovalenko","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2015,3,4]]},"reference":[{"key":"e_1_2_6_1_2","first-page":"518","volume-title":"Chemistry of Heterocyclic Compounds, Vol.\u200524","year":"2008"},{"key":"e_1_2_6_2_2","doi-asserted-by":"publisher","DOI":"10.1039\/b413750g"},{"key":"e_1_2_6_3_2","doi-asserted-by":"publisher","DOI":"10.1135\/cccc19940222"},{"key":"e_1_2_6_4_2","first-page":"189","volume":"52","author":"Shiba S. 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