Abstract
A series of 1-carboxyphenothiazines bearing nitrogen mustard was synthesized, characterized, and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. The results showed that compounds 5h, 5i and 5j found most active with percentage inhibition of 96, 91, and 92, respectively, at minimum inhibitory concentration (MIC) of <6.25 μg/mL, among the synthesized compounds. Whereas compounds 5a, 5b, 5c, 5d, 5e, 5f and 5g exhibited considerable antitubercular activity with percentage inhibition of 71, 75, 79, 54, 55, 68, and 66, respectively, at MIC of >6.25 μg/mL. The structures of synthesized compounds were elucidated by various spectroscopic tools like IR, 1H NMR, 13C NMR, mass and elemental analysis.
Keywords: Antitubercular activity, 1-carboxyphenothiazines, Minimum inhibitory concentration, Mycobacterium tuberculosis, Nitrogen mustard, Spectroscopic tools.
Letters in Drug Design & Discovery
Title:Synthesis and Characterization of 1-carboxyphenothiazine Derivatives Bearing Nitrogen Mustard as Promising Class of Antitubercular Agents
Volume: 10 Issue: 10
Author(s): V.B. Kataria, M.J. Solanki, A.R. Trivedi and V.H. Shah
Affiliation:
Keywords: Antitubercular activity, 1-carboxyphenothiazines, Minimum inhibitory concentration, Mycobacterium tuberculosis, Nitrogen mustard, Spectroscopic tools.
Abstract: A series of 1-carboxyphenothiazines bearing nitrogen mustard was synthesized, characterized, and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. The results showed that compounds 5h, 5i and 5j found most active with percentage inhibition of 96, 91, and 92, respectively, at minimum inhibitory concentration (MIC) of <6.25 μg/mL, among the synthesized compounds. Whereas compounds 5a, 5b, 5c, 5d, 5e, 5f and 5g exhibited considerable antitubercular activity with percentage inhibition of 71, 75, 79, 54, 55, 68, and 66, respectively, at MIC of >6.25 μg/mL. The structures of synthesized compounds were elucidated by various spectroscopic tools like IR, 1H NMR, 13C NMR, mass and elemental analysis.
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Kataria V.B., Solanki M.J., Trivedi A.R. and Shah V.H., Synthesis and Characterization of 1-carboxyphenothiazine Derivatives Bearing Nitrogen Mustard as Promising Class of Antitubercular Agents, Letters in Drug Design & Discovery 2013; 10 (10) . https://dx.doi.org/10.2174/15701808113109990022
DOI https://dx.doi.org/10.2174/15701808113109990022 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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