Dual evaluation of some novel chalcone annulated pyrazolines as anti-in lammatory and antimicrobial agents via in-silico target study on cyclooxygenase-2 Production and Hosted by (original) (raw)

2019, INTERNATIONAL JOURNAL OF RESEARCH IN PHARMACEUTICAL SCIENCES

A novel series of chalcone bearing pyrazoline moieties were (P1 to P7) synthesized and characterized by various analytical techniques. The anti-in lammatory studies showed the compounds P1, P2, P5, and P6 have produced the noteworthy inhibition on protein denaturation (81.39-96.57 %) when compared to standard 98.17% whereas, the antiproteinase activity was in the range of 84.55-90.44 % when compared to the standard, 95.95 %. The compounds, P1, P2, P5 (2-Cl, 4-Cl &-NO 2 substituent) bearing electron-withdrawing groups and the compounds P3 & P6 (4-N(CH 3) 2 &-OH sub-stituent) possessing electron-donating group in its phenyl ring system exhibited the prominent activity. Further, to explore the molecular mechanism, the in-silico docking study against COX-2 enzyme was performed. The compounds were also screened for their antibacterial activities. Among them, the compounds P1, P2, P3, P5 and P6 showed the signi icant antibacterial activity against both gram-positive and gram-negative pathogen such as, Bacillus cereus, Staphylococcus aureus, Serratia marcescens and Staphylococcus typhi with maximum zone of inhibition within the range of 12-14 mm and 19-25 mm for 100 and 200 µg/ml concentrations respectively when compared to that of standard drug Gentamycin, whose ranges between 15-18 mm and 25-28 mm correspondingly.