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.

A simple and sensitive reverse phase high performance liquid chromatographic method was developed and successively validated for the estimation of Canagliflozin. In the new method, Canagliflozin separation was carried out by the nonpolar inertsil ODS-3 (250 × 4.6 mm, 5μ) column with a mobile phase composition of Ammonium acetate buffer (pH-4.5) and Acetonitrile in the ratio of 30:70% v/v. Canagliflozin was determined at 252 nm using UV detection and the compound was eluted at the retention time of 4.5 min. As per International Conference on Harmonization (ICH) guidelines, the method was validated and the parameters were precision, accuracy, linearity, limit of detection, limit of quantitation and robustness. The chromatographic method was accurate, linear, specific, precise and robust. The results of method concluded that the proposed RP-HPLC method is useful, convenient and reliable in regular analysis of Canagliflozin in bulk and its formulation

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