期刊
FUTURE MEDICINAL CHEMISTRY
卷 9, 期 15, 页码 1701-1708出版社
Newlands Press Ltd
DOI: 10.4155/fmc-2017-0098
关键词
4-aminoquinoline; antitubercular activity; ferrocenyl chalcone
资金
- University Grants Commission (UGC), New Delhi, India, under UGC-JRF Fellowship [23/12/2012(ii)EU-V]
- Science and Engineering Board (SERB), New Delhi [EMR/2015/001687]
Aim: Tuberculosis is responsible for 9.6 million infections and 1.5 million deaths in 2015. The development of multidrug-resistant and extensively drug-resistant strains has impeded the development of effective antitubercular therapy. Results/methodology: The present manuscript describes the synthesis of a series of 4-aminoquinoline-ferrocenylchalcone conjugates via Cu-promoted Huisgen's azide-alkyne cycloaddition reaction and evaluation of their antitubercular activities against mc(2)6230 strain of Mycobacterium tuberculosis. The conjugate 11j proved to be the most potent of the synthesized conjugates with a minimum inhibitory concentration (MIC99) value of 30 mu M and proved to be noncytotoxic against HeLa cells. Conclusion: The synthesized conjugates can act as starting point for the development of new antitubercular agents. Synthesis and antitubercular evaluation of 1H-1,2,3-triazole-tethered 4-aminoquinoline-ferrocenylchalcone conjugates. [GRAPHICS] .
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