Archive \ Volume.5 2014 Issue 2

SYNTHESIS AND ANTIINFLAMMATORY ACTIVITY OF NOVEL PYRIMIDINO BENZOTHIAZOLE AMINE DERIVATIVES

Anuradha Doma , Ravindra Kulkarni , Achaiah Garlapati , Palakodety Radha Krishna
Abstract

(Benzothiazol-2yl) acetonitrile have been reported to exhibit inhibition of c-Jun N-terminal kinase which is known to play a vital role in cell death (apoptosis) and inflammation. A detail study of SAR of (Benzothiazol-2yl) acetonitrile compounds revealed that Benzothiazol-2-ylidinyl and pyrimidine scaffolds are important for the JNK inhibitory activity. This study intended to hydrolyze the nitrile group in to acid to afford (Benzothiazol-2yl)-2-(2-substituted pyrimidin-4yl) acetic acids (4a-z) and observe for their anti-inflammatory properties. All the compounds have been synthesized by following known literature procedures and characterized by 1H NMR, IR, and Mass and subjected to screening for the anti-inflammatory activity by carrageenan induced in vivo rat paw edema model. Compounds 4h and 4q were found to possess significant activity amongst all the compounds.


[PDF]