Dinakaran, Murugesan ; Senthilkumar, Palaniappan ; Yogeeswari, Perumal ; China, Arnab ; Nagaraja, Valakunja ; Sriram, Dharmarajan (2008) Antimycobacterial activities of novel 2-(sub)-3-fluoro/nitro-5,12-dihydro-5-oxobenzothiazolo[3,2-a]quinoline-6-carboxylic acid Bioorganic & Medicinal Chemistry, 16 (6). pp. 3408-3418. ISSN 0968-0896
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Official URL: http://linkinghub.elsevier.com/retrieve/pii/S09680...
Related URL: http://dx.doi.org/10.1016/j.bmc.2007.11.016
Abstract
Various 2-(sub)-3-fluoro/nitro-5,12-dihydro-5-oxobenzothiazolo[3,2-a]quinoline-6-carboxylic acid derivatives were synthesized from 2-aminothiophenol by a five-step reaction, evaluated for in-vitro and in-vivo antimycobacterial activities against Mycobacterium tuberculosis H37Rv (MTB), multi-drug resistant Mycobacterium tuberculosis (MDR-TB), and Mycobacterium smegmatis (MC2), and also tested for the ability to inhibit the supercoiling activity of DNA gyrase from M. smegmatis. Among the thirty-four synthesized compounds, 2-(3-(diethylcarbamoyl)piperidin-1-yl)-)-3-fluoro-5,12-dihydro-5-oxobenzothiazolo[3,2-a]quinoline-6-carboxylic acid (7l) was found to be the most active compound in vitro with MIC of 0.18 and 0.08 μM against MTB and MTR-TB, respectively. Compound 7l was found to be 2 and 570 times more potent than isoniazid against MTB and MDR-TB, respectively. In the in-vivo animal model 7l decreased the bacterial load in lung and spleen tissues with 2.78 and 3.12 - log 10 protections, respectively, at the dose of 50 mg/kg body weight.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | Antimycobacterial Activity; Antitubercular Activity; Tuberculosis; Benzothiazoloquinolone |
| ID Code: | 26991 |
| Deposited On: | 08 Dec 2010 12:53 |
| Last Modified: | 25 Jan 2011 15:25 |
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