Kalaiyarasi, P (2019) Design, Synthesis, Characterization and Biological Evaluation of Some Novel Indole Derivatives as Anti Tubercular Agents Targeting Glutamine Synthetase 1. Masters thesis, College of Pharmacy, Madras Medical College, Chennai.
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Abstract
Glutamine synthetase I enzyme is the critical enzyme for the survival and growth for Mycobacterium tuberculosis is chosen as the potential drug target. ➢Molecules were designed and docked against Glutamine synthetase I enzyme 3ZXR protein using Autodock® 4.2.1 software. ➢Molecules with good docking score were screened for insilico toxicity by using OSIRIS® software and evaluation of drug likeness by MOLINSPIRATION software. ➢The selected compounds were synthesized and labeled as PK1, PK2, PK3, PK4, PK5. ➢Purity of the synthesized compounds were justified by its sharp melting point and TLC. ➢Further the synthesized compounds were characterized by IR, LC-MS, H1NMR. ➢Biological evaluation is done by MICROPLATE ALAMAR BLUE ASSAY ➢Compounds PK2 and PK4 showed activity at 1.6 μg/ml concentrations which are comparable to the activity of the standard drugs Pyrazinamide, Streptomycin, Ciprofloxacin which are active at 3.125μg/ml,6.25μg/ml,3.125μg/ml concentrations. CONCLUSION ➢A series of Schiff bases of isatin derivatives were designed, docked, synthesized and evaluated against Glutamine synthetase 1 enzyme which is critical for the survival and growth of MTB. ➢The Minimum Inhibitory Concentration of the synthesized compounds ranges from 50-1.6μg/ml. ➢The work concludes that the Compounds Compounds PK2 and PK4 showed activity at 1.6 μg/ml concentrations which are comparable to the activity of the standard drugs Pyrazinamide, Streptomycin, Ciprofloxacin which are active at 3.125μg/ml,6.25μg/ml,3.125μg/ml concentrations. ➢Further, structural refinement of the synthesized compounds is expected to yield promising molecules against the pathogen MTB.
| Item Type: | Thesis (Masters) |
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| Additional Information: | 261715702 |
| Uncontrolled Keywords: | Design, Synthesis, Characterization, Biological Evaluation, Indole Derivatives, Anti Tubercular Agents, Glutamine Synthetase 1 |
| Subjects: | PHARMACY > Pharmaceutical Chemistry |
| Depositing User: | Ramakrishnan J |
| Date Deposited: | 11 May 2022 10:43 |
| Last Modified: | 11 May 2022 10:43 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/20018 |
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