Abstract

SYNTHESIS, CHARACTERIZATION, ANTI-INFLAMMATORY, ANALGESIC ACTIVITY AND INSILCO DOCKING STUDIES OF NOVEL BENZOTHIAZOLE DERIVATIVES

Archana Rao*, Sumer Singh, Khaja Pasha

ABSTRACT

In existing study, 3-(6-substituted-benzo[d]thiazol-2-ylimino)-1-(phenyl sulfonyl) indolin-2-one was synthesized by conventional method and all the derivatives were purified recrystallization, Column chromatographically technique’s and characterized by IR, 1H NMR and mass spectral data. The biological potentials of the newly synthesized benzothiazole derivatives are evaluated for them in-vitro anti-inflammatory and analgesic activities carried out by standard protocol. The compound 4j and 4l are showed good Anti-inflammatory activity, whereas others exhibited significant activities. The compound 4h and 4m are has showed maximum analgesic activity compare with pentazocine as a standard drug. Dock scores of all the synthesized derivatives ranged from -4.943 (compound 4b) to -3.369 (compound 4f). Compounds 4k (dock score -4.80) and 4c (dock score -4.260) possessed two hydrogen bonds each with THR 830 and LYS 721 amino acids. Hydrophobic interactions were observed with PHE 699 residue in compounds 4k (benzothiazole moiety) and between compound 4b (benzothiazole moiety) and LYS 721.

Keywords: benzo[d]thiazol, and Diclofenac sodium, Pentazocine, inflammatory activity, analgesic activity.