| DOI: 10.29090/psa.2020.01.018.0045 | Pharm Sci Asia 2020; 47(1), 30-36 |
Synthesis and bioevaluation of some new N-substituted pyranophenothiazinesThi-Thuan Nguyen1*,Hanh Dufat2,Sylvie Michel2
1 Hanoi University of Pharmacy, 13-15 Le Thanh
Tong, Ha Noi, Vietnam
2 Laboratoire de Pharmacognosie, UMR/CNRS
8638, Universit? Paris Descartes, 75006 Paris,
France
Tuberculosis is a dangerous infectious disease. Because of the enlargement of multidrug-resistant strains (MDR-TB), the need of new drugs becomes more important. In the last research, 2 pyranophenothiazine series had been synthesized and bio-evaluated. Herein, eight N-substituted pyranophenothiazine derivatives from 2 series were designed, synthesized and evaluated for their antituberculosis activities. The designed compounds were prepared by alkylation reactions and all synthesized compounds were confirmed by analysis of NMR and MS spectra. Antimycobacterial activity of the synthesized compounds on Mycobacterium bovis BCG had been determined using the microdilution resazurin assay - The results showed that 4 compounds exhibited a mild inhibiting activity on the tested tuberculosis strains. These structural requirements will be taken into account for the design of further analogues in pyranophenothiazine series.
Keyword:
Pyranophenothiazine; Chromene; Antituberculosis; Phenothiazine derivatives
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