| Title: | Green Synthesis, Cytotoxicity and Antimicrobial Activities of Some New Pyrazolines, Pyrimidines and Naphthyridines Based on 1,3-Di(thien-2-yl)prop-2-en-1-one Using Choline Chloride-Urea Mixture As A Deep Eutectic Solvent |
| Authors: | Enas A. Mohamed, Abdelmotaal Abdelmajeid, Mohamed S. Behalo, Aly A. Alya and Kaouser A. Hebash |
| Year: | 2022 |
| Keywords: | Chalcone; deep eutectic solvent; pyrazoline; pyrimidine; antitumor activity; antimicrobial activity |
| Journal: | Egyptian Journal of Chemistry |
| Volume: | 65 |
| Issue: | 4 |
| Pages: | 651 - 663 |
| Publisher: | National Information and Documentation Centre (NIDOC), Academy of Scientific Research and Technology, ASRT |
| Local/International: | International |
| Paper Link: | |
| Full paper | Enas A. Mohamed_EJCHEM-Volume 65-Issue 4- Page 651-663.pdf |
| Supplementary materials | Not Available |
| Abstract: |
An efficient and facile green synthesis of chalcone derivatives 1a-d was achieved by treatment of aromatic aldehydes with 2-acetylthiophene in the presence of choline chloride-urea mixture as a deep eutectic solvent. Chalcone 1a was used as a reactive key precursor to design a series of bio-active heterocycles such as pyrimidine, pyrazoline, pyridine, pyridopyrimidine and naphthyridine. The Structural formula of derivatives were confirmed and characterized by their elemental analyses and spectral data (IR, MS, 1H NMR, 13C NMR). In addition, the synthesized derivatives were evaluated for their antimicrobial activities, it was found that compounds 3, 8 and 9a exhibited potent antifungal activity in comparison with the standard drug. Cytotoxicity against breast cancer (MCF7) was screened also and most compounds showed low to moderate activity. The results of the viral screening against HBV of selected compounds indicated that compounds (9b, 15), 8, (3, 6), and 5 showed moderate viral replication inhibition. |
