Arathi K N, Sindhu T J, Vishnu M V, Basith M A, Anitha S V, Annlisa Roy, Arundhathi T, Ashly George, Asish S
Arathi K N1*, Sindhu T J1, Vishnu M V2, Basith M A3, Anitha S V1, Annlisa Roy1, Arundhathi T1, Ashly George1, Asish S1
1Department of Pharmaceutical Chemistry, Sanjo College of Pharmaceutical Studies, Vellapara, Kuzhalmannam, Palakkad, Kerala - 678702, India.
2Department of Pharmaceutical Chemistry, Chemists College of Pharmaceutical Sciences and Research, Puthencruz, Ernakulam, Kerala - 682308, India.
3Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER) S.A.S. Nagar, Sector 67, S.A.S. Nagar, Mohali, Punjab -160062, India.
Volume - 16,
Issue - 3,
Year - 2023
In this work we aimed to design synthesis and evaluate the N-Mannich bases of pyrazole. A novel series of N-Mannich bases of pyrazole analogues were designed and synthesized with an effort to overcome the increasing antibiotic resistance. Tyrosyl-tRNA synthetase (TyrRS) comprises an N-terminal domain, which has the fold of the class I aminoacyl-tRNA synthetases. Computational Autodock 4.2 tools will be employed in this study for docking of pyrazole ligand molecules against Tyrosyl-tRNA synthetase (TyrRS) of Escherichia coli (PDB code: 1x8x) and Staphylococcus aureus (PDB code: 1jil.pdb). Molinspiration server was used for lead optimization. The ligand molecules were subjected to molecular docking studies with enzyme Tyrosyl-tRNA synthetase. The molecular docking studies are supported to compare in-vitro antibacterial activity by the use of binding energy of the docked ligand molecules. The newly synthesized compounds were characterized by UV, IR and various physico-chemical methods. Further, the antibacterial activity of N-Mannich bases of pyrazole compounds were assessed with zone of inhibition by agar well diffusion method using gram negative bacterial strain Escherichia coli and gram-positive strain staphylococcus aureus. These same compounds were subjected to find the antifungal activity against Aspergillus fumigates and Aspergillus Niger.
Cite this article:
Arathi K N, Sindhu T J, Vishnu M V, Basith M A, Anitha S V, Annlisa Roy, Arundhathi T, Ashly George, Asish S. Synthesis, Molecular Docking and Characterization of Pyrazole N-Mannich Base Derivatives as Antimicrobial Agents. Research Journal of Pharmacy and Technology 2023; 16(3):1047-2. doi: 10.52711/0974-360X.2023.00175
Arathi K N, Sindhu T J, Vishnu M V, Basith M A, Anitha S V, Annlisa Roy, Arundhathi T, Ashly George, Asish S. Synthesis, Molecular Docking and Characterization of Pyrazole N-Mannich Base Derivatives as Antimicrobial Agents. Research Journal of Pharmacy and Technology 2023; 16(3):1047-2. doi: 10.52711/0974-360X.2023.00175 Available on: https://rjptonline.org/AbstractView.aspx?PID=2023-16-3-11
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