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Objective: The objective of the paper was to synthesize and characterize new derivatives of thiazole-based pyrazole derivatives and evaluate them for the antitubercular activity.
\n\nMaterial and methods: The pyrazole derivatives have been synthesized by the two steps process in that first step pyrazole based carbothioamide compounds was synthesized and it further reacted with 3-(2-bromoacetyl)-2H-chromen-2-one to from the final compounds. Total Fourteen compounds have been synthesized and characterized by IR, 1HNMR, elemental analysis and mass spectral analysis. The final Compounds (TP-1 to TP-14) have been evaluated for antitubercular activity by two Ex-vivo method i.e. LRP assay and MABA method.
\n\nResult and Discussion: IR analysis of compound TP-1 to TP-14 showed the occurrence of the characteristics peak at 3415-3420 (-NH), 1717-1721 (-C=O) and 1627 (-C=N). The 1H-NMR spectrum shown a singlet peak at δ 8.53, due to the chromen-2-one-4H proton. The characteristic peak of -NH proton was attributed at δ 12.02-12.03. The MABA method depicted the efficacy of compound by MIC value in µg/ml; five compounds i.e. TP-8 (1.75), TP-3 (1.75), TP-9 (2.50), TP-10 (2.25), and TP-1 (2.25) have shown lowest MIC among all other compounds and it was similarly active with the standard anti-TB drug Isoniazid (MIC value 1.25 µg/ml). Luciferase reporter phase assay result data suggested that at 100µg/ml concentration, 10 compounds (TP-1, TP-2, TP-3, TP-4, TP-5, TP-8, TP-9, TP-10 TP-11 and TP-12) shown the potent anti-tubercular activity. Structure activity relationship (SAR) of the compound indicated that 4-chlorophenyl substitution at 3rd position of pyrazole with 4-chlorophenyl, 4-nitrophenyl and 4-methylphenyl substitution at 1st position of pyrazole have enhance the anti-tubercular potential.
\n\nKeywords: Anti-tubercular activity, LRP assay, MABA method, pyrazole, Thiazole
", "publication_date": "2022-07-05", "publisher": "Zenodo", "resource_type": { "id": "publication-article", "title": { "de": "Zeitschriftenartikel", "en": "Journal article" } }, "rights": [ { "description": { "en": "The Creative Commons Attribution license allows re-distribution and re-use of a licensed work on the condition that the creator is appropriately credited." }, "icon": "cc-by-icon", "id": "cc-by-4.0", "props": { "scheme": "spdx", "url": "https://creativecommons.org/licenses/by/4.0/legalcode" }, "title": { "en": "Creative Commons Attribution 4.0 International" } } ], "title": "SYNTHESIS AND CHARACTERIZATION OF NEW DERIVATIVES OF PYRAZOLE AND SCREENED FOR THEIR ANTITUBERCULAR POTENTIAL" }, "parent": { "access": { "owned_by": { "user": 159385 } }, "communities": {}, "id": "6798418", "pids": { "doi": { "client": "datacite", "identifier": "10.5281/zenodo.6798418", "provider": "datacite" } } }, "pids": { "doi": { "client": "datacite", "identifier": "10.5281/zenodo.6798419", "provider": "datacite" }, "oai": { "identifier": "oai:zenodo.org:6798419", "provider": "oai" } }, "revision_id": 2, "stats": { "all_versions": { "data_volume": 64651680.0, "downloads": 45, "unique_downloads": 43, "unique_views": 47, "views": 50 }, "this_version": { "data_volume": 64651680.0, "downloads": 45, "unique_downloads": 43, "unique_views": 46, "views": 49 } }, "status": "published", "updated": "2022-07-05T13:48:41.853063+00:00", "versions": { "index": 1, "is_latest": true } }