European Journal of Biomedical and Pharmaceutical Sciences

SYNTHESIS, CHARACTERIZATION, DOCKING AND BIOLOGICAL ACTIVITIES OF SOME NOVEL SCHIFF BASES OF PYRAZOLINE DERIVATIVES FROM CHALCONE

Kalpana Devi* and Monica Kachroo

ABSTRACT

The substituted aldehydes and ketones were reacted to obtain chalcones using the well known Claisen Schmidt condensation. The chalcone derivatives were further cyclized to pyrazoline carbaldehyde using hydrazine hydrate and formic acid. The cyclized pyrazoline carbaldehyde derivatives were subjected to Schiff base reactions with p-amino pyridine. Various invitro biological activities were carried out like anti-TB by MABA method, antibacterial by MIC method, anti-inflammatory by BSA method and antioxidant by DPPH and NO radical scavenging methods. 5(a) with hydroxyl and chloro substitutents on the benzene rings showed activity with a MIC value of 25 μg/ml against Mycobacterium tuberculosis. Most of the derivatives have shown good activity against P.aeruginosa and S.pneumoniae. Compounds 5(b) and 5(c) having Br, OH and Cl substitutents respectively exhibited higher percentage inhibition when compared to the standard (89% and 90% at 100 and 200 μg/ml respectively and indomethacin 90% and 91% at the same concentration). However it was observed that the % inhibition exhibited by DPPH method is high as compared to the NO method for both the standard as well as for the test samples. The potential of these molecules as mycobacterial, antibacterial and antiinflammatory agents were predicted using molecular docking studies

Keywords: Pyrazoline carbaldehyde, Schiff base, anti-TB, antibacterial, anti-inflammatory, antioxidant, docking.