期刊
MOLECULES
卷 26, 期 8, 页码 -出版社
MDPI
DOI: 10.3390/molecules26082110
关键词
1; 3; 4-oxadiazoles; N-Mannich bases; antimicrobial activity; anti-proliferative activity
资金
- Deanship of Scientific Research at Princess Nourah bint Abdulrahman University through the Research Groups Program [RGP-1442-0010-4]
A series of novel N-Mannich base compounds were synthesized in this study, with the piperazinomethyl derivatives showing broad-spectrum antibacterial activities. Some compounds also demonstrated potent anti-proliferative activity against Gram-positive bacteria and various cancer cell lines.
The reaction of 5-(3,4-dimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione 3 with formaldehyde solution and primary aromatic amines or 1-substituted piperazines, in ethanol at room temperature yielded the corresponding N-Mannich bases 3-arylaminomethyl-5-(3,4-dimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thiones 4a-l or 3-[(4-substituted piperazin-1-yl)methyl]-5-(3,4-dimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thiones 5a-d, respectively. The in vitro inhibitory activity of compounds 4a-l and 5a-d was assessed against pathogenic Gram-positive, Gram-negative bacteria, and the yeast-like pathogenic fungus Candida albicans. The piperazinomethyl derivatives 5c and 5d displayed broad-spectrum antibacterial activities the minimal inhibitory concentration (MIC) 0.5-8 mu g/mL) and compounds 4j, 4l, 5a, and 5b showed potent activity against the tested Gram-positive bacteria. In addition, the anti-proliferative activity of the compounds was evaluated against prostate cancer (PC3), human colorectal cancer (HCT-116), human hepatocellular carcinoma (HePG-2), human epithelioid carcinoma (HeLa), and human breast cancer (MCF7) cell lines. The optimum anti-proliferative activity was attained by compounds 4l, 5a, 5c, and 5d.
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