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SYNTHESIS, CHARACTERISATION AND BIOLOGICAL EVALUATION OF SOME PYRAZOLONE DERIVATIVES

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Abstract (2. Language): 
The synthetic part involves the formation of N'-({1-[(4substituted phenyl)carbonyl]-3-methyl-5-oxo-4,5-dihydro- 1Hpyrazol-4-yl}methyl)pyridinecarbohydrazide from the substituted acid hydrazide. The structures of the final compounds were established on the basis of IR, 1H-NMR and MASS spectral data. Drug likeness was determined by Molinspiration software program. Parameters related to drug likeness of the derivatives were established on the basis of Lipinski’s rule of 5. The molecular properties were calculated from suitable computational tools. All of the derivatives showed a zero violations of the rule of 5 which indicates good bioavailability. The positive bioactivity score of the derivative were also in agreement with their probability of drug likeness. The entire synthetic derivative was evaluated for their antimicrobial studies. Most of the derivatives were showed good activity towards gram positive bacteria and less activity towards gram negative bacteria. Some of the derivatives showed moderate activity against tested fungi.
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