Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis and Anti-Inflammatory Activity of Fused 1,2,4-triazolo-[3,4-b] [1,3,4]thiadiazole Derivatives of Phenothiazine

Author(s): S. Maddila, S. Gorle, M. Singh, P. Lavanya, S. B. Jonnalagadda.

Abstract:

A new series of 10-((6-(substitutedphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl)methyl)-10H-phenothiazine derivatives (7a-k) moiety are prepared using intermediate compound 5-((10H-phenothiazin-10-yl)methyl)-4-amino-4H-1,2,4-triazole-3-thiol (5). The structures of newly synthesized compounds were confirmed on the basis of their 1H NMR, 13C NMR, LCMS mass, FT-IR and elemental analysis data results. All the compounds were screened for their significant anti-inflammatory activity of inhibition in paw oedema at 3h and 5h respectively, compared to the standard drug indomethacin. The Compounds 7k and 7d showed potent activity, while compounds 7g, 7b, 7j, 7i and 7c exhibited significant activity when compared to the standard drug, due to the presence of mild electron withdrawing groups such as difluoro, fluorine, chlorofluoro, nitro and chlorine derivatives which are attached to the benzene rings.

Keywords: Anti-inflammatory activity, Phenothiazine, Synthesis, 1, 2, 4-Triazole-3-thiol, 1, 2, 4-Triazolo[3, 4-b][1, 3, 4]thiadiazole.

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Article Details

VOLUME: 10
ISSUE: 10
Year: 2013
Page: [977 - 983]
Pages: 7
DOI: 10.2174/15701808113109990034
Price: $58