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1,3,4-Oxadiazole N -Mannich Bases: Synthesis, Antimicrobial, and Anti-Proliferative Activities by Lamya H. Al-Wahaibi; Ahmed A. B. Mohamed; Samar S. Tawfik; Hanan M. Hassan; Ali A. El-Emam is a Chemistry article available to read on EtoBox.

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The reaction of 5-(3,4-dimethoxyphenyl)-1,3,4-oxadiazole-2(3__H__)-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(3__H__)-thiones **4a**–**l** or 3-[(4-substituted piperazin-1-yl)methyl]-5-(3,4-dimethoxyphenyl)-1,3,4-oxadiazole-2(3__H__)-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 μg/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 line

Who reads 1,3,4-Oxadiazole N -Mannich Bases: Synthesis, Antimicrobial, and Anti-Proliferative Activities?

Author

Lamya H. Al-Wahaibi; Ahmed A. B. Mohamed; Samar S. Tawfik; Hanan M. Hassan; Ali A. El-Emam

Publisher

MDPI AG

Published

2021

Language

EN

Field

Chemistry (Life Sciences)