Synthesis Some Novel Pyrazolo[3,4-D]Pyrimidine Clubbed With Phenothiazine Nucleus and Their Biological Evaluation

Authors

  • Nirul V. Gothi  Arts, Science & R. A. Patel commerce college, Bhadran, Gujarat, India

Keywords:

Pyrazolopyrimidines, Phenothiazines, Antitubercular Activity, BACTEC Assay

Abstract

The reaction of 2-(methylthio)-10H-phenothiazine (1) with hydrazine hydrate afforded 1-(10H-phenothiazin-8-yl)hydrazine (2) and that with ethyl acetoacetate afforded 3-methyl-1-(10H-phenothiazin-8-yl)-1H-pyrazol-5(4H)-one (3), which was condensed with different aromatic aldehydes and thiourea to give a series of 4,5-dihydro-4-(aryl)-3-methyl-1-(10H-phenothiazin-8-yl)-1H-pyrazolo[3,4-d]pyrimidine-6-thiols (4a-h). The compounds 4a-h were characterized by FT-IR, 1H NMR, 13C NMR, mass spectra and elemental analysis. All the newly synthesized compounds 4a-h were evaluated for their antitubercular activity against Mycobacterium tuberculosis H37Rv using radiometric BACTEC and broth dilution assay methods. 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 MIC of <6.25 μg/mL. While, 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 μg/mL.

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International Journal of Scientific Research in Science, Engineering and Technology

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Published

2014-12-30

Issue

Volume 1, Issue 1, -2014

Section

Research Articles

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How to Cite

[1]
Nirul V. Gothi, " Synthesis Some Novel Pyrazolo[3,4-D]Pyrimidine Clubbed With Phenothiazine Nucleus and Their Biological Evaluation, International Journal of Scientific Research in Science, Engineering and Technology(IJSRSET), Print ISSN : 2395-1990, Online ISSN : 2394-4099, Volume 1, Issue 1, pp.192-197, -2014.