New 1,3-oxazolo[4,5-c]quinoline derivatives: synthesis and evaluation of antibacterial and antituberculosis properties.
A new class of fused oxazoloquinoline derivatives was synthesized starting from 2-bromo-1-phenylethanones 1a-b through multi-step reactions. The newly synthesized compounds were evaluated for their in vitro antibacterial against Escherichia coli (ATTC-25922), Staphylococcus aureus (ATTC-25923), Pseudomonas aeruginosa (ATCC-27853) and Klebsiella pneumoniae (recultured) and antituberculosis activity against Mycobacterium tuberculosis H37Rv (ATCC 27294). Preliminary results indicated that most of the compounds demonstrated very good antibacterial and antituberculosis activities which are comparable with the first line drugs. Compounds 6a, 6c, 6g, 6j, 6k and 6n emerged as the lead antitubercular agents with MIC, 1 microg/mL and 99% bacterial inhibition while eight compounds, viz., 5a, 15k, 6a, 6c, 6g, 6j, 6k and 6n were found to be more potent than INH (MIC: 1.5 microg/mL) with MIC 1 microg/mL.
Eswaran
Sumesh
S
Anthem Biosciences Pvt. Ltd., 49 Bommasandra Industrial Area, Bommasandra, Bangalore 560099, Karnataka, India.
Adhikari
Airody Vasudeva
AV
Ajay Kumar
R
R
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004926:Escherichia coli / Q000187:drug effects; D007711:Klebsiella pneumoniae / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D010080:Oxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D013211:Staphylococcus aureus / Q000187:drug effects
D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D010080:Oxazoles; D011804:Quinolines; C037219:quinoline