Enamino Barbiturates as Antiproliferative and Antimicrobial Agents: Studies on Synthesis, Biological Activities, and Molecular Modeling

Author:

Shtaiwi Majed1ORCID,Abu Sarhan Ayman H.1,Aljaar Nayyef1ORCID,Shtaiwi Amneh2ORCID,Abu‐Sini Mohammad3ORCID,Alwahsh Mohammad3ORCID,Hamadneh Lama3ORCID,Malakar Chandi C.4ORCID,Abu‐Safieh Kayed A.1ORCID

Affiliation:

1. Department of Chemistry, Faculty of Science The Hashemite University P.O. Box 330127 Zarqa 13133 Jordan

2. Faculty of Pharmacy Middle East University Queen Alia Airport Street Amman 11118 Jordan

3. Faculty of Pharmacy Al-Zaytoonah University of Jordan P.O. Box 130 Amman 11733 Jordan

4. Department of Chemistry National Institute of Technology Manipur, Langol Imphal, Manipur 795004 India

Abstract

AbstractIn the present study, the aimed enamines 3 aj were synthesized with yield ranging between 65 and 81 % by the reaction of 5‐((dimethylamino)methylene)‐1,3‐dimethylpyrimidine‐2,4,6(1H,3H,5H) ‐trione (2) with different amines at room temperature (25 °C). The structures of all synthesized compounds were characterized using different spectroscopic techniques. Molecular docking studies of the new compounds 3 aj were carried out with human estrogen receptor (hER) enzyme to evaluate their activities as an effective drug molecules. It was investigated that the compounds 3 b, 3 e, 3 f and 3 j revealed the best binding affinities. All new compounds were evaluated towards antifungal activities, which conceded that the compound 3 e displayed a remarkable antifungal activity compared to the Fluconazole and Nystatin, and its Minimum Inhibitory Concentration (MIC) found to be 0.011 mM, while for Fluconazole the MIC value exhibited at 0.046 mM. Additionally, the toxicity for the new compounds found to be better than tamoxifen on MCF‐7 cells and among these molecules, the compound 3 e displayed the lowest IC50 value.

Funder

Hashemite University

Publisher

Wiley

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