The infectious diseases caused by antimicrobials pathogens are difficult, harmful, and sometimes impossible to treat. Therefore, design new drugs to treat antimicrobial infections is the biggest challenge for modern medicine. 2-Thioxo-4-imidazolidinone is used for the synthesis of a wide variety of new substituted imidazolidinone derivatives. In this study, we designing eight novel compounds derived for the 2-thioxo-4-imidazolidinones (5ah). The preparation was in two steps via Micheal addition of phenyl hydrazide (2a), 4-methyl phenyl hydrazide 2b on N-substituted maleimides 1a-d in ethanol, and the second step by reaction of maleimide derivatives with cyclohexyl isothiocyanate 4 in acetonitrile. The chemical structures of the compounds were identified using FT-IR, 1 H-NMR, 13 C-NMR, and mass spectra, as well as the melting point. The antibacterial and antifungal evaluation was carried out to target their activities. Compound N-(5-(2-((4-chlorophenyl)amino)-2-oxoethyl)-3cyclohexyl-4-oxo-2-thioxoimidazolidin-1-yl) benzamide (5b) exhibited antibacterial activity toward Staphylococcus aureus and Pseudomonas aeruginosa with equal minimum inhibitory concentration (MIC) values of 25 mg/mL. Compounds N-(3-cyclohexyl-4-oxo-5-(2-oxo-2-(phenylamino)ethyl)-2-thioxoimidazolidin-1-yl) benzamide (5a), N-(5-(2-((4-chlorophenyl)amino)-2-oxoethyl)-3-cyclohexyl-4-oxo-2-thioxoimidazolidin-1-yl) benzamide (5b), N-(5-(2-((4-bromophenyl)amino)-2-oxoethyl)-3-cyclohexyl-4-oxo-2-thioxo imidazolidin-1-yl) benzamide (5c), and N-(3-cyclohexyl-4-oxo-5-(2-oxo-2-(phenylamino)ethyl)-2-thioxoimidazolidin-1-yl)-4methyl benzamide (5e) exhibited antifungal activity toward Candida albicans, while all compounds exhibited antifungal activity toward Aspergillus niger except for compound 5h, with various MIC values. In conclusion, the results demonstrate that the new compounds have to promise as antifungal agents. Moreover, compound 5b could develop as an antibacterial agent.

Four new 2-thiohydantoin derivatives (4a-d) were synthesized from the reaction of maleimide derivatives (3a-d) with phenylisothiocyanate. The structures of synthetic compounds were characterized using Fourier-transform infrared spectroscopy (FT-IR), 1 H-and 13 C-nuclear magnetic resonance (NMR) spectroscopy, and mass spectrometry. The antioxidant activity of the synthesized compounds showed inactive 4b and 4c compounds, moderately active 4a, and strongly active 4d, compared with vitamin C as positive control (IC50 values = 1.380, 1.726, 4.147, 8.085, and 9.826 µM, respectively). Antibacterial and antifungal activities of compounds showed that only compound 4b had an effect on Pseudomonas aeruginosa, Candida albicans, and Aspergillus niger species.

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Based on vanillin and diamine compounds (ortho phenylene diamine, meta phenylene diamine, 3,4- diamine toluene), derivation of two new Schiff base ligands (L1 and L2) was done, after which synthesis and treatment with Co (II) chloride was performed at a metal-to-ligand ratio of 1:1 to get two new complexes, i.e. [CoL3(H2O)2]Cl2 and [CoL1(H2O)2]Cl2. These complexes and ligands were characterized by employing NMR, IR, atomic absorption, UV visible absorption, molecular weight determination, molar conductance, and magnetic measurement techniques. As per the data, the ligands were found to be bidentate ligands that were linked to two azomethine nitrogen sites. It was suggested that these complexes were paramagnetic electrolyte compounds that possessed coordination number four. Screening of the ligands and metal complexes was done to assess their antimicrobial activities against gram-negative and gram-positive bacteria, which was found to show biological activity. Calculations using quantum chemistry were done to examine the molecule geometry. The investigation includes several quantum chemical characteristics derived from frontier molecular orbitals. Keywords: Schiff bases, transition metal complexes, vanillin, diamine aromatic compounds, antibacterial activity, DFT study.

MTT assay and flowcytometry analysis were used to examine the anti-liver (HepG2) and anti-breast cancer (MCF-7) activities of twelve compounds derived from 2-thioxo-4-imidazolidine. The compounds 5a-h and 7f demonstrated significant anticancer activity against breast cancer cells, while the compounds 5a, ab, and 5d-h demonstrated significant anticancer activity against liver cancer cells, with varying IC50 values as compared to Cisplatin as the positive control. Among these compounds, we chose 5a, 5d, and 5h to detect cell cycle phases and late apoptosis. Compound 5a arrested MCF-7 cells in the S phase, while compound 5d arrested cells in the G1 phase. Compound 5a arrested S phase HepG2 cells, compound 5d arrested S phase cells, and compound 5h arrested G2 phase HepG2 cells. Compound 5a had a higher ratio of late apoptosis than compounds 5d and 5h on both cancer cells. Finally, the development of these compounds as new anti-breast and anti-liver agents warrants further research to understand the mechanism of action, especially against breast cancer.