Recently, some prostate cancer patients have acquired resistance to the second -generation drugs (anzalutamide and apalutamide) prescribed for the treatment of this disease due to the emergence of the F876L mutation, which represents a challenge to modern medicine. In this study, a new series of 2-thiohydantoin derivatives were prepared through the reaction of different derivatives of maleimide (1c-4c) with isothiocyanate derivatives. The prepared compounds were diagnosed using FT-IR,1H-NMR ,13C-NMR, Mass spectra. The prepared series compounds has been studied against prostate cancer cells. The MTT assay was used to determine the activity of the prepared compounds against prostate cancer cells. The data indicated, depending on the IC50 values, that some of the prepared compounds have anti-prostate cancer activity. The results indicate that compounds 1d and 2d have good anti-prostate cancer activity compared to the rest of the compounds. The prepared series of compounds were also studied against selected types of bacteria and fungi, as the results showed that some of the compounds in the series had anti-bacterial and anti-fungal activity.
Objectives: Six different Schiff bases were synthesized from ampicillin and amoxicillin with isatin, 5-bromoisatin, and 5-nitroisatin. Methods: Ampicillin and Amoxicillin are linked directly through their α-amino groups to the acyl side chain with isatin and isatin derivatives by nucleophilic addition using glacial acetic acid as a catalyst. Results: chemical structures of these Schiff bases were confirmed using FTIR, 1H NMR and elemental microanalysis. The antibacterial activity was evaluated by measuring minimum inhibitory concentration (MIC) values and showed various degrees of antibacterial activities when compared with parent drugs. Compounds 1a and 2b, which are the Schiff bases of ampicillin and amoxicillin with isatin, showed very
... Show MoreWith the aim of developing potential antimicrobials, a series of novel Ciprofloxacin methylene isatin derivatives incorporating different aromatic aldehydes were synthesized and characterized by FTIR, 1H NMR, Mass spectroscopy and bases of elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique. A majority of compounds were showing activity against several of the microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds is discussed. From comparisons of the compounds, 3c was determined to be the most active compound.
This study focused on the synthesis of novel polymers incorporating the 1,3,4-oxadiazole ring. Four polymers were specifically prepared by blending polymers (6-9) with polyvinyl alcohol (PVA) in defined ratios, resulting in the formation of blended polymers (10-13). The synthesized polymers were characterized using Fourier Transform Infrared (FTIR) spectroscopy and proton nuclear magnetic resonance (1H-NMR). The results showed that the structure aligned with the proposed synthetic polymers. Furthermore, the physical and thermal properties were studied using scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC). Additionally, the biological activity was examined against two s
... Show MoreThis study focused on the synthesis of novel polymers incorporating the 1,3,4-oxadiazole ring. Four polymers were specifically prepared by blending polymers (6-9) with polyvinyl alcohol (PVA) in defined ratios, resulting in the formation of blended polymers (10-13). The synthesized polymers were characterized using Fourier Transform Infrared (FTIR) spectroscopy and proton nuclear magnetic resonance (1H-NMR). The results showed that the structure aligned with the proposed synthetic polymers. Furthermore, the physical and thermal properties were studied using scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC). Additionally, the biological activity was examined against two s
... Show MoreThe new ligand [N1,N4-bis((1H-benzo[d]Glyoxalin-2-yl)carbamothioyl)Butanedi amide] (NCB) derived from Butanedioyl diisothiocyanate with 2-aminobenz imidazole was used to prepare a chain of new metal complexes of Cr(III), Mn(II), Co(II), Ni(II), Cu(II), Pd(II), Ag(I), Cd(II) by general formula [M(NCB)]Xn ,Where M= Cr(III), n=3, X=Cl; Mn(II), Co(II), Ni(II), Cu(II), Pd(II), Cd(II) ,n=2 , X=Cl; Ag(I), n=1, X=NO3. Characterized compounds on the basis of 1H, 13CNMR (for (NCB), FT-IR and U.V spectrum, melting point, molar conduct, %C, %H, %N and %S, the percentage of the metal in complexes %M, Magnetic susceptibility, thermal studies (TGA),while its corrosion inhibition for mild steel in Ca(OH)2 solution is studied by weight loss. These measureme
... Show MoreIn this research, 5- membered heterocyclic compounds as oxazolidine-5-one J1-J5 derivatives were prepared using primary aromatic amine, aromatic carbonyl compounds and chloroacetic acid. By combining primary aromatic amines and aromatic carbonyl compounds, Schiff's bases were synthesized. Schiff bases are used with the chloroacetic acid compound to prepare oxazolidine-5-one J1-J5 derivatives. The compounds J1-J5 were described using NMR spectroscopy and FT-IR. .The biological efficacy was evaluated according to maximum inhibitory concentrations (MICs) toward Staphyloccoccus aureus and Esherichia coli. The best MIC was 210 μg ml-1 for J4 against the two pathogenic bacteria, while J1, J4, and J1 did not show any inhibitory effect against all
... Show MoreAbstract: New copper(II) complexes with mixed ligand benziloxime (BOxH) and furfural-dehydeazine (FA) using classical (with and without solvent) and microwave heating methods have been prepared. The resulting complexes have been characterized using physico-chemical techniques. The study suggested that the ligands formed neutral complexes had general formulas [Cu(FA)(BOXH)(Ac)2] and [Cu(FA)(BOX)(OH)] in neutral (or acidic) and basic medium, respectively. Accordingly, hexa-coordinated mono-nuclear complexes have been investigated by this study and having distorted octahedral geometry. The effect of laser have been studied on solid ligands and solid complexes, no effect have been observed on most compounds through the results of melting poin
... Show MoreAntibiotic resistance is the major growing threat facing the pharmacological treatment of bacterial infections. Therefore, bioprospecting the medicinal plants could provide potential sources for antimicrobial agents. Mimusops, the biggest and widely distributed plant genus of family Sapotaceae, is used in traditional medicines due to its promising pharmacological activities. This study was conducted to elucidate the antimicrobial effect of three unexplored Mimusops spp. (M. kummel, M. laurifolia and M. zeyheri). Furthermore, the mechanisms underlying such antibacterial activity were studied. The Mimusops leaf extracts revealed significant antibacterial activities against the five tested bacter
... Show MoreAASAH Enass J Waheed, Shatha MH Obaid, Research Journal of Pharmaceutical, Biological and Chemical Sciences, 2019 - Cited by 5