57164-59-7Relevant academic research and scientific papers
Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors
Medapi, Brahmam,Meda, Nikhila,Kulkarni, Pushkar,Yogeeswari, Perumal,Sriram, Dharmarajan
, p. 877 - 885 (2016/05/24)
In this study we have designed p-phenylene diamine linked acridine derivative from our earlier reported quinoline-aminopiperidine hybrid MTB DNA gyrase inhibitors with aiming more potency and less cardiotoxicity. We synthesized thirty six compounds using four step synthesis from 2-chloro benzoic acid. Among them compound 4-chloro-N-(4-((2-methylacridin-9-yl)amino)phenyl)benzenesulphonamide (6) was found to be more potent with MTB DNA gyrase super coiling IC50of 5.21 ± 0.51 μM; MTB MIC of 6.59 μM and no zHERG cardiotoxicity at 30 μM and 11.78% inhibition at 50 μM against mouse macrophage cell line RAW 264.7.
