4.5 Article

1H-1,2,3-Triazolyl-substituted 1,3,4-oxadiazole derivatives containing structural features of ibuprofen/naproxen: Their synthesis and antibacterial evaluation

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 21, 页码 5212-5217

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.09.059

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Ibuprofen; Naproxen; 1,2,3-Triazole; Azide; Alkyne; Antibacterial activity

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1H-1,2,3-Triazolyl-substituted 1,3,4-oxadiazole derivatives containing structural features of ibuprofen/naproxen were synthesized for the first time using a Cu catalyzed azide-allcyne cycloaddition (CuAAC) strategy. An optimized reaction condition was established for this purpose and twenty new compounds were synthesized using this methodology. Several of these compounds showed good to reasonable antibacterial activities when tested against three gram-positive and three gram-negative species. The compound 4m i.e. N-(2-chloropheny1)-2-(44(5-(1-(6-methoxynaphthalen-2-yl)ethyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)acetamide showed promising activities across both the species. (C) 2016 Elsevier Ltd. All rights reserved.

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