Literature DB >> 24333580

Synthesis and evaluation of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-(2-(4-substitutedpiperazin-1-yl)acetyl)piperazin-1-yl)quinoline-3-carboxylic acid derivatives as anti-tubercular and antibacterial agents.

Narva Suresh1, Hunsur Nagendra Nagesh1, Janupally Renuka2, Vikrant Rajput3, Rashmi Sharma3, Inshad Ali Khan3, Chandra Sekhar Kondapalli Venkata Gowri4.   

Abstract

A series of twenty two novel 1-cyclopropyl-6-fluoro-4-oxo-7-(4-substitutedpiperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid analogues were synthesized, characterized ((1)H NMR, (13)C NMR and LCMS) and screened for their in vitro anti-tubercular and antibacterial activity. Many of these compounds exhibited MIC values in the range 7.32-136.10 μM against Mycobacterium tuberculosis H37Rv. Eight compounds were further subjected to cytotoxic studies. Furthermore, the title compounds were screened for antibacterial activity against Staphylococcus aureus ATCC 29213 (gram positive) and Escherichia coli ATCC 25922 (gram negative) bacteria. Many of these compounds exhibited MIC values in the range 0.44-34.02 μM. Compound 3f was found to be the most active with an MIC of 0.44 and 0.8 μM respectively against both the strains. In general, the antibacterial activity of title compounds was more prominent.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Anti-tubercular activity; Antibacterial activity; Cytotoxicity; Fluoroquinolone; Supercoiling assay

Mesh:

Substances:

Year:  2013        PMID: 24333580     DOI: 10.1016/j.ejmech.2013.10.055

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  2 in total

1.  Application of 2,4-bis(halomethyl)quinoline: synthesis and biological activities of 2,4-bis(benzofuran-2-yl)- and 2,4-bis(aroxymethyl)quinolines.

Authors:  Yang Li; Qiqi Xu; Zhiyuan Li; Wentao Gao; Yu Chen
Journal:  Mol Divers       Date:  2019-03-20       Impact factor: 2.943

2.  Potential antibacterial and antifungal activities of novel sulfamidophosphonate derivatives bearing the quinoline or quinolone moiety.

Authors:  Ismahene Bazine; Samira Bendjedid; Abbes Boukhari
Journal:  Arch Pharm (Weinheim)       Date:  2020-12-07       Impact factor: 4.613

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.