Synthesis, anti-microbial activity, and cytotoxicity of novel 1-[5-[6-[(2-benzoylbenzofuran-5-yl)methyl]-2-oxo-2H-chromen-3-yl]thiazol-2-yl]urea derivatives
| Autor: | P. Jalapathi, B. Shankar, Karunakar Rao Kudle, Modhumpuram Nagamani, Bharath Gandu |
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| Rok vydání: | 2016 |
| Předmět: |
biology
Triphosgene 010405 organic chemistry General Chemistry Carbon-13 NMR 010402 general chemistry biology.organism_classification Antimicrobial 01 natural sciences Medicinal chemistry 0104 chemical sciences HeLa chemistry.chemical_compound Biochemistry chemistry Cell culture Urea Proton NMR Cytotoxicity |
| Zdroj: | Monatshefte für Chemie - Chemical Monthly. 148:999-1009 |
| ISSN: | 1434-4475 0026-9247 |
| DOI: | 10.1007/s00706-016-1838-z |
| Popis: | A series of novel 1-[5-[6-[(2-benzoylbenzofuran-5-yl)methyl]-2-oxo-2H-chromen-3-yl]thiazol-2-yl]urea derivatives were synthesized by the reaction of 3-(2-aminothiazol-5-yl)-6-[(2-benzoylbenzofuran-5-yl)methyl]-2H-chromen-2-one with various substituted amines and triphosgene, in the presence of a base. The chemical structures of newly synthesized compounds were elucidated by 1H NMR, 13C NMR, IR, MS, and HRMS spectral data. The synthesized compounds evaluated for their inhibitory effects as anti-microbial activity and cytotoxicity. Most of the compounds exhibited a promising anti-microbial activity against the selected Gram-positive and Gram-negative bacterial strains at MIC values ranging from 0.071 to 0.199 μM and fungal pathogen was moderate to be good. The in vitro cytotoxicity testing of the title compounds was performed against cervical cancer (HeLa) cell lines. In the preliminary MTT cytotoxicity studies, the results have shown that there are a few of the synthesized compounds which exhibit a significant cytotoxicity at microliter concentration were found to non-toxic, their IC50 values ranging from 49.322/15 to 52.715/15 mm3. |
| Databáze: | OpenAIRE |
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