Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry

Abstract

Synthesis, In Silico and In Vitro evaluation of some novel 5-[2-phenyl vinyl]-pyrazole and pyrazoline derivatives

Author(s): K. N. V. Chenchu Lakshmi, M. Venkatesh, J. Hareesh, B. Srinivasa Raju and B. Anupama

A series of novel pyrazole and pyrazoline derivatives were prepared from substituted benzaldehydes and acetone as starting materials through dibenzalacetone as intermediate. These intermediates on reaction with hydrazines in acidic media, finally converted into corresponding pyrazoles and pyrazolines. The synthesized compounds were characterized by their physical properties, IR, H1 NMR, C13 NMR spectral studies. The Insilco methods were used to evaluate the drug likeness of compounds, and to assess the inhibition of derivatives against 5 subtypes of cytochrome P450. The compounds 2,5,8 showed inhibition against nuclear , ligand and kinase receptors .The synthesised derivatives were also evaluated for anti bacterial activity against both gram positive and gram negative organisms with standard streptomycin and were found to have inhibition against gram positive organisms.


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