Synthesis and antibacterial activity of new lactone 1,4-dihydroquinoline derivatives

AbstractIn this work, a series of lactone 1,4-dihydroquinoline derivatives4 were efficiently synthesized and characterized by1H and13C NMR. The synthesized compounds were evaluated for their in vitro antibacterial activity against the bacterial strainsPorphyromonas gingivalis,Prevotella nigrescens,Streptococcus mitis, andStreptococcus sanguinis and againstMycobacterium tuberculosis, Mycobacterium avium andMycobacterium kansasii. The results revealed that the evaluated compounds were more active against Gram negative bacteria. Compounds4ba,4bb,4bg,4bi,4bn,4ch, and4ci displayed moderate antibacterial activity againstP. gingivalis.4bi was the most active compound against the three strains ofMycobacterium. Based on structure –activity relationship studies, we observed that the presence of a nitro group on the benzylic ring and a methylenedioxy group on the dihydroquinoline ring enhanced the antibacterial activity of the derivatives.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research