A novel series of 1,3,5-trisubstituted pyrazole derivatives were synthesized by the cycloaddition reaction between the electron rich N-substituted aryl hydrazones and nitro-olefins. Different N-substituted aryl hydrazones (1a-j) on reacting with 4-methyl-β-nitrostyrene (2) in ethylene glycol or trifluoroethanol-trifluoro acetic acid mixture (for acid stable hydrazones) at 120 ºC, yielded various 1,3,5-trisubstituted pyrazoles (3a-j). The final products were characterized by spectral analysis using Mass, NMR and IR spectroscopy. All the products were assessed for their anti-inflammatory, analgesic and antipyretic activities on Swiss albino rats. All the compounds (3a-j) exhibited noteworthy defence against inflammation, nociception and hyperthermia. Compounds (3e and 3h) disclosed better antiinflammatory, analgesic and antipyretic activities while compound 3c had highest anti-inflammatory activity compared to the standard nimesulide.

Background: Pyrazole derivatives have been reported to possess numerous pharmacological activities viz., antiinflammatory, antipsychotic and etc. Our group have disclosed that pyrozole benzamides display potent antibacterial and antitubercular activities. Objective: Synthesis of new pyrazole acetamides which possess hydrazone group to be evaluated for antitubercular activity. Methods: The key intermediate 5-aminopyrazole was synthesized with known procedure which is then converted into chloroacetamide. This compound than resulted hydrazine derivative and finally the converted in to aromatic hydrazones. All the compounds were screened for anti-tubercular activity. Result: All the synthesized compounds have been characterized by their spectral data obtained and subjected for anti-tubercular activity. Among all the twenty tested compounds, three compounds, 5a5, 5b5 and 5b7 have demonstrated MIC value of 3.12 μg/mL against MTB H37Rv. Docking studies revealed important hydrogen bonding interactions with InhA. Conclusion: Three compounds 5a5, 5b5 and 5b7 were found to be most potent among the series of compounds. Docking studies of compounds explained the presence of hydrogen bonding and π-π stacking interactions with InhA. Further synthesis of more such derivatives with optimized groups would produce compounds with more potent anti-tubercular activity.

An accurate RP-HPLC method developed for the estimation of Neratinib in bulk and tablet dosage form. The method is and validated for parameters linearity, accuracy, suitability, specificity, precession, LOD, LOQ and robustness. An Altima column (150 mm × 4.6 mm × 5μ) used for chromatographic separation within a runtime of 6 min. The mobile phase buffer (monopotassium phosphate) and acetonitrile (60:40 v/v) with 0.1% formic acid is used. The flow rate maintained at 1.0 ml/min with the effluents monitored at 215 nm. The Neratinib analyzed at retention time of 4.001. The concentration linear over 30-180μg/ml with regression equation y = 6065.6x + 795.43 and regression co-efficient 0.999.