Thatavarthi Padmini, Darna Bhikshapathi, Kandagatla Suresh, Ravindra Kulkarni* and Bigala Raj Kamal Pages 1 - 8 ( 8 )
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.
Pyrazolylacetamides, Antitubercular, Synthesis, Characterization, Molecular docking, InhA.
Mewar University, Chittorgarh, Rajasthan, Teegala Ram Reddy College of Pharmacy, Pragathi Colony, Meerpet, Hyderabad- 500097, Telangana, Vijaya College of Pharmacy, Hayatnagar, Hyderabad-501511, Telangana, Hyderabad, Bharati Vidyapeeth's Poona College of Pharmacy, Erandwane, Pune-411038, Maharashtra, Mewar University, Chittorgarh, Rajasthan