Synthesis and antibacterial activity of (1-aryl-1, 2, 3-triazol-4-yl) methyl esters of morpholine-3-carboxylic acid

Abstract

A series of new 1,2,3-triazolyl methyl ester of morpholine-3-carboxylic acid analogues were designed and synthesized employing click chemistry by using Huisgen 1,3 dipolar cyclo addition reaction between propargyl ester of morpholine-3-carboxylic acid and aryl azides. The starting materials propargyl ester and aryl azides were synthesized by well established methods. The newly synthesized compounds were characterized by spectral studies. The compounds were screened for antibacterial activity. Majority of the compounds exhibited promising activity and one of them (6i) displayed more activity than standard drug against S. paratyphi-B. A molecular docking study showed hydrogen bonds and pi-interactions with the compound. Our data indicate that these derivatives may present promising anti-bacterial agents. Graphical Abstract: [Figure not available: see fulltext.]