1414875-82-3Relevant academic research and scientific papers
Synthesis and 3D-QSAR analysis of 2-chloroquinoline derivatives as H 37 RV MTB inhibitors
Khunt, Ranjan C.,Khedkar, Vijay M.,Coutinho, Evans C.
, p. 669 - 684 (2013)
Frequency of tuberculosis is progressively increasing worldwide. New emerging strains of bacilli that are emerging are resistant to the currently available drugs which make this issue more alarming. In this regard, a series of substituted quinolinyl chalcones, quinolinyl pyrimidines, and pyridines were synthesized and evaluated for their antitubercular activity in vitro against Mycobacterium tuberculosis H37RV. To establish the role of the 2-chloroquinoline nucleus as a pharmacophoric group and study its influence on the antimycobacterial activity, a 3D-QSAR study based on CoMFA and CoMSIA was undertaken on this set of 2-chloroquinoline derivatives. Statistically significant models that are able to well correlate the antimycobacterial activity with the chemical structures of the 2-chloroquinolines have been developed. The contour maps resulting from the best CoMFA and CoMSIA models were used to identify the structural features relevant to the biological activity in this series of analogs. Further analysis of these interaction-field contour maps also showed a high level of internal consistency. The information obtained from the field 3-D contour maps may be fruitfully utilized in the design of more potent 2-chloroquinoline-based analogs as potential antitubercular candidates. A series of 1 chloroquinoline bearing pyridine and pyrimidine ring system and fluoro/bromo at C-3 and C-6 of the quinoline ring were synthesized and evaluated for their antimycobacterial activity. The MIC data of antitubercular activity was performed for 3D QSAR analysis.
Synthesis and characterization of some new quinoline based derivatives endowed with broad spectrum antimicrobial potency
Desai, Nisheeth C.,Rajpara, Kiran M.,Joshi, Vivek V.
supporting information, p. 6871 - 6875,5 (2020/09/02)
The synthesis of a novel series of 2-(5-(2-chloro-6-fluoroquinolin-3-yl)-3- (aryl)-4,5-dihydro-1H-pyrazol-1-yl)thiazol-4(5H)-ones (4a-l) and N-(4-(2-chloro-6-fluoroquinolin-3-yl)-6-(aryl)pyrimidin-2-yl) -2-morpholinoacetamides (7a-l) are described in the present paper. The chemical structures of compounds have been elucidated by IR, 1H NMR, 13C NMR and mass spectral data. Antimicrobial activity was measured against Escherichia coli (MTCC 443), Pseudomonas aeruginosa (MTCC 1688), Staphylococcus aureus (MTCC 96), Streptococcus pyogenes (MTCC 442), Candida albicans (MTCC 227), Aspergillus niger (MTCC 282) and Aspergillus clavatus (MTCC 1323) by serial broth dilution. Evaluation of antimicrobial activity showed that several compounds exhibited greater activity than reference drugs and thus could be promising new lead molecules.
