Microwave assisted stereoselective synthesis and antibacterial activity of new fluoroquinolinyl-beta-lactam derivatives

摘要

A series of quinoline ring substituted N-(3-chloro-2-(2-fluoro-quinolin-3-yl)-4-oxoazetidin-1-yl)-octanamides were synthesized from chloroacetyl chloride, octanoic acid, (2-fluoro-quinolin-3-yl-methylene)-hydrazides, and triethylamine using microwave irradiation as well as conventional heating. The reaction time can be brought down from hours to minutes with improved yields using microwave irradiation compared to conventional heating. The compounds were tested for their in vitro antibacterial activity against 2253-Corynebacterium rubrum, 2340-Enterobacter, 2491-Erwinia herbicola, K-12-E coil, and 2873-Z. mobilis. and found to possess activities comparable with or superior to the standard drug ampicillin. [References: 17]