Assembly of Benzothiazine and Triazole in a Single Molecular Entity: Synthesis of -Oxicam Derived Novel Molecules as Potential Antibacterial/ Anti-cancer Agents
| Autor: | Suryapeta Srinivas, Khagga Mukkanti, B. Sridhar, Pramod Kumar Dubey, Venkanna Banothu, Papigani Neeraja, Sarbani Pal |
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| Rok vydání: | 2020 |
| Předmět: |
1
2 3-Triazole Triazole Antineoplastic Agents Chemistry Techniques Synthetic Benzothiazine Benzothiadiazines 010402 general chemistry 01 natural sciences chemistry.chemical_compound Drug Discovery medicine Humans Cytotoxicity Pharmacology 010405 organic chemistry Chemistry Drug discovery General Medicine Triazoles Combinatorial chemistry Anti-Bacterial Agents 0104 chemical sciences Oxicam Azide Antibacterial activity medicine.drug |
| Zdroj: | Mini-Reviews in Medicinal Chemistry. 20:929-940 |
| ISSN: | 1389-5575 |
| Popis: | Background: Benzothiazine derivatives, because of their various biological activities have attracted particular attention in Med Chem and drug discovery efforts. The synthetic modifications of 1,2-benzothiazine 1,1-dioxides have been undertaken in order to explore and identify novel compounds or new analogues possessing promising biological activities. In our effort we have designed -oxicam derived bezothiazine-1,2,3-triazole derivatives as potential antibacterial agents. Methods: These compounds were synthesized via a multi-step sequence involving the Cu catalyzed azide- alkyne cycloaddition (CuAAC) as a key step. The CuAAC proceeded at room temperature in DMF to afford 26 novel molecules in good (70-90%) yields. Results: All these compounds were tested for their antibacterial properties against four strains of bacterial microorganisms and subsequently cytotoxic properties against lung and colon cancer cell lines. The compound 4e showed activities against majority of the bacterial species used (nearly comparable to amoxicillin, ciprofloxacin and ofloxacin against P. vulgaris) whereas 4d and 4f showed cytotoxicities selective towards cancer cells. Conclusion: The present bezothiazine-1,2,3-triazole framework represents a new template for the identification of novel and potent antibacterial/anticancer agents. |
| Databáze: | OpenAIRE |
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