2008
DOI: 10.3998/ark.5550190.0009.223
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Design, synthesis, characterization and antitubercular activity of some 2-heterocycle-substituted phenothiazines

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 H 37 Rv.

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Cited by 47 publications
(5 citation statements)
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“…Phenothiazines and related compounds, including tranquilizers [7] and drugs with anti-inflammatory [8], antimalarial [9], antipsychotic [10], antimicrobial [11], antitubercular [12,13], antitumor [14e16], antihistaminic [17] and analgesic [18] properties, have found widespread use in medicinal chemistry. Among these, those that act as antihistaminic and antipsychotic agents are the ones most exploited therapeutically.…”
Section: Introductionmentioning
confidence: 99%
“…Phenothiazines and related compounds, including tranquilizers [7] and drugs with anti-inflammatory [8], antimalarial [9], antipsychotic [10], antimicrobial [11], antitubercular [12,13], antitumor [14e16], antihistaminic [17] and analgesic [18] properties, have found widespread use in medicinal chemistry. Among these, those that act as antihistaminic and antipsychotic agents are the ones most exploited therapeutically.…”
Section: Introductionmentioning
confidence: 99%
“…Numerous applications of phenothiazine heterocycles and their derivatives as drugs have stimulated the continued study of this class of organo-sulfur compounds. [1][2] In medicine, phenothiazine derivatives possess a wide range of biological activities including antibacterial, 3 antifungal, 4 antipsychotic, 5 anti-inflammatory, 6 antiparkinsonian, 7 anti-tubercular, 8 anticonvulsant, 9 and cardiovascular 10 activities. In addition to the main neuroleptic action of phenothiazine family, their antitumor activities are profusely reported.…”
Section: Introductionmentioning
confidence: 99%
“…Pyrimidine heterocyclic core has great value in medicinal chemistry since it comprises the base for thiamine, uracil, and cytosine nitrogen bases which are the building blocks of the nucleic acids (12,13). Furthermore, pyrimidine derivatives have registered their importance in the development of various pharmaceuticals of broad spectra of therapeutical activities such as anti-microbial (14), anti-viral, anti-HIV (15,16) anti-tubercular (17,18) anti-malarial (19)(20)(21). The derivatives of 1,2,3,4-tetrahydropyrimidine-2-thiones have been reported to be calcium channel blockers (22), antitumors (23), antidepressant (24), antibacterial (25), and antifungal (26,27).…”
Section: Introductionmentioning
confidence: 99%