AN EFFICIENT AND GREEN APPROACH FOR THE SYNTHESIS OF INDOLYL-PYRIMIDINE DERIVATIVES AND INVESTIGATION OF BIOLOGICAL ASSAYS

SYNTHESIS OF INDOLYL-PYRIMIDINE DERIVATIVES AND INVESTIGATION OF BIOLOGICAL ASSAYS

Abstract

The present work describes the synthesis of biologically active molecules chalcone (3a-d) and indolyl- pyrimidine derivatives (5a-d). The novel synthesized compounds were characterized by physiochemical methods like melting point, TLC and spectral data such as IR, ¹H NMR, ¹³C NMR and mass spectroscopy. The present approach offers the simplicity of the workup procedure, low cost and mild reaction conditions. The RSA best result was obtained by compound 3d (at the all the concentrations, when compared to standard AA (94.21 %). The compound 3b showed potent activity (62.5µg/mL) against Escherichia coli (MTCC-723), 3b showed equipotent activity (125µg/mL) against all others tested bacteria. The antifungal activity of compound 3a showed potent activity (62.5 µg/mL) against Aspergillus niger (MTCC-281). The compound 3a showed excellent activity against M. tuberculosis H37Rv (MIC 3.125 µg/ml) than the standards pyrazinamide and streptomycin (MIC 3.125 and 6.25 µg/mL).