Anoop, P (2012) Desing Molecular Docking, Syntheseis and Evaluation of Some novel Heterocyclic Analogues of 2-Substituted Benzimidazole as potent Antimicrobial, Analgesic, Anti Inflammatory Agents. Masters thesis, K M College of Pharmacy, Madurai.
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Abstract
In the present study, the main motto was to develop new chemical entities as potential anti-inflammatory, analgesic and antimicrobial agents by chemical modification of the 2nd position of prepared benzimidazole by different heterocyclic rings. In our attempt, firstly 3-(1H-benzimidazol-2-yl) propanoic acid was prepared. Suitable heterocyclics which give potent ligands were identified by the carboxylic group present in the prepared 3-(1Hbenzimidazol- 2-yl)propanoic acid with the heterocyclics like pyridazine-3,4- dione, 2,3-dihydrophthalazine-1,4-dione, 1,3,4-oxadiazole. Furthermore, it has been reported in literature that certain compounds bearing these nucleus possesses a wide spectrum of activities like analgesic, anti-inflammatory, anticonvulsant, antipyretic, antihypertensive, antiviral, antituberculosis, antimicrobial, anticancer activities etc. then identification and characterization of synthesized compounds by different methods like physical properties (M.P, Solubility, Thin layer chromatography) and spectral analysis (IR, NMR). Finally selective pharmacological activities like Antimicrobial, Analgesic and Anti-inflammatory activities need to examine. Various pyridazine-3,6-dione, 2,3-dihydrophthalazine-1,4-dione, 1,3,4- oxadiazole derivatives of 3-(1H-benzimidazol-2-yl)propanoic acid were designed and synthesized with the aim of developing better analgesic anti-inflammatory molecules with antimicrobial activity. The results generated in this study leads to the following conclusions. Molecular docking studies reveal that all the designed ligands 1- 8 possess very good binding ability in COX-2 and 14 α- demethylase enzymes. All the test compounds exhibit significant analgesic activities against acetic acid induced writhing reflux. All the test compounds exhibit significant anti-inflammatory activity in carrageenan induced rat paw edema method. The test compounds A, F, E, H showed high degree of antibacterial activity when compared with standard Amikacin and test compounds A, C, G showed high degree of antifungal activity against when compared with standard Ketoconazole. The result obtained support the statement that newly synthesized heterocyclic analogues of benzimidazole can be considered as good analgesic anti-inflammatory agent with antimicrobial activity, however further structural modification are planned to increase the activity of this series to obtain a clinically useful antimicrobial, analgesic and anti-inflammatory agent.
| Item Type: | Thesis (Masters) |
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| Uncontrolled Keywords: | Syntheseis; Heterocyclic; Benzimidazole; oxadiazole |
| Subjects: | PHARMACY > Pharmaceutical Chemistry |
| Depositing User: | Ravindran C |
| Date Deposited: | 17 Aug 2017 05:26 |
| Last Modified: | 17 Aug 2017 05:26 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/2642 |
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