A series of phenothiazine clubbed pyrazolo[3,4-d]pyrimidines have been synthesized by using the Biginelli multi-component cyclocondensation reaction and their ability to inhibit growth of Mycobacterium tuberculosis in vitro have been determined. The results show that compounds 4b, 4d, and 4f exhibited excellent anti-tubercular activity with percentage inhibition of 93, 91, and 96, respectively, at a minimum inhibitory concentration (MIC) of\6.25 lg/ml, whereas compounds 4a, 4c, 4e, 4g, and 4h exhibited moderate to good anti-tubercular activity with percentage inhibition of 75, 68, 74, 54, and 63, respectively at a MIC of [6.25 lg/ml.
Some novel 2-heterocycle-substituted phenothiazines having a pyrazolo [3,4-d]pyrimidine nucleus have been synthesized by using the Biginelli multi-component cyclocondensation reaction. The products were characterized by FT-IR, 1 H NMR, 13 C NMR, mass spectra and elemental analysis. The products were evaluated for their antitubercular activity against Mycobacterium tuberculosis H 37 Rv.
A new and facile synthetic route is proposed for the synthesis of some novel phenothiazines (5a-5g) based on the reaction of 2-amino substituted benzenethiols with p-tert-butyl phenol in good yield. The newly synthesized compounds were characterized by IR, 1 H NMR and mass spectral studies. Their antimicrobial activities against three strains of bacteria: Bacillus subtilis, Bacillus megaterium, Escherichia coli, and two strains of fungi: Aspergillus niger and Aspergillus oryzae, were investigated.
4,5-Dihydro-1H-pyrazolo[3,4-d]pyrimidine Containing Phenothiazines as Antitubercular Agents. -Novel pyrazolopyrimidine derivatives (IV) (11 examples) are synthesized in high yield via a modified Biginelli multicomponent reaction and screened for their antimycobacterial activities. New compound (IVd) shows most pronounced activity against Mycobacterium tuberculosis with minimum inhibitory concentration, making it more potent than the reference drug isoniazid. -(SIDDIQUI*, A. B.; TRIVEDI, A. R.; KATARIA, V. B.; SHAH, V. H.; Bioorg. Med. Chem. Lett. 24 (2014) 6, 1493-1495, http://dx.
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