Original articleSynthesis and antimycobacterial activities of novel 6-nitroquinolone-3-carboxylic acids

Add time:09/03/2019    Source:sciencedirect.com

Various 1-(substituted)-1,4-dihydro-6-nitro-4-oxo-7-(sub-secondary amino)-quinoline-3-carboxylic acids were synthesized from 2,4-dichlorobenzoic acid by six step synthesis. The compounds were evaluated for antimycobacterial in vitro and in vivo against Mycobacterium tuberculosis H37Rv (MTB), multi-drug resistant Mycobacterium tuberculosis (MDR-TB) and Mycobacterium smegmatis (MC2) and also tested for the ability to inhibit the supercoiling activity of DNA gyrase from M. smegmatis. Among the 48 synthesized compounds, 7-(4-((benzo[d][1,3]dioxol-5-yl)methyl)piperazin-1-yl)-1-cyclopropyl-1,4-dihydro-6-nitro-4-oxoquinoline-3-carboxylic acid (8c) was found to be the most active compound in vitro with MIC of 0.08 and 0.16 μM against MTB and MDR-TB, respectively. In the in vivo animal model 8c decreased the bacterial load in lung and spleen tissues with 2.78 and 4.15-log 10 protections, respectively, at the dose of 50 mg/kg body weight.

We also recommend Trading Suppliers and Manufacturers of 1-METHYL-4-OXO-1,4-DIHYDRO-QUINOLINE-3-CARBOXYLIC ACID (cas 18471-99-3). Pls Click Website Link as below: cas 18471-99-3 suppliers

Prev:15N, 13C and 119Sn NMR and other spectroscopic studies of 8-quinolinol, its O- and N-methyl derivatives, and chelate di- and tri-organotin(IV) complexes
Next:Design, synthesis and biological evaluation of 4-aminoquinoline-guanylthiourea derivatives as antimalarial agents)