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

作者：Neeraja Papigani; Srinivas Suryapeta; Mukkanti Khagga; Dubey Pramod Kumar; Pal Sarbani^*

来源：Bioorganic & Medicinal Chemistry Letters, 2016, 26(21): 5212-5217.

DOI：10.1016/j.bmcl.2016.09.059

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

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.

• 出版日期2016-11-1