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.
Objective: Tuberculosis, known in short as TB, is considered to be a global crisis caused by Myco bacterium tuberculosis, and which continues to be a serious challenge to public health world wide especially in the developing countries. A serious problem related to tuberculosis is the development of drug resistant strains. Methods: Present study describes the synthesis of eight novel derivatives of 1,3,4-thiadiazole derivatives and in vitro evaluation of their anti tubercular activity against Mycobacterium tuberculosis H37 Rv strain by alamar blue assay. Pyrazinamide and Streptomycin were the standards, used for the evaluation. Results: Among the eight compounds synthesized one derivative was found to be active against the strain tested. All the other derivatives tested exhibited negligible activity against the strain. Conclusion: It can be concluded that novel 1, 3, 4-thiadiazole derivatives can be developed as novel agents in the fight against TB.
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