Abstract

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 H37 Rv.

Highlights

  • The chemistry of nitrogen-sulfur heteroatom containing aromatic compounds is becoming more popular as an area of research

  • A slight variation in the substitution pattern on the phenothiazine nucleus often causes a marked difference in activities and phenothiazines with various substituents are being synthesized and tested for activities in search of better medicinal agents

  • Several pyrimidine derivatives containing a phenothiazine nucleus were synthesized at reflux temperature

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Summary

Introduction

The chemistry of nitrogen-sulfur heteroatom containing aromatic compounds is becoming more popular as an area of research. Phenothiazines and related compounds have shown diverse biological activities including as tranquilizers,[1] anti-inflammatory,[2] antimalarial,[3] antipsychotropic,[4] antimicrobial,[5] antitubercular,[6,7] antitumour[8,9,10] and stimulation of the penetration of anticancer agents via the blood-brain barrier. Some of these derivatives have been reported to exhibit significant anticancer activities[13,14] and great interest has arisen in the design and synthesis of new phenothiazines to explore their anticancer activities.

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