Creatinine and Schiff`s bases are well known for their diverse range of biological activities and are thought to be emerging and useful therapeutic targets for the treatment of several diseases. The present work was aimed at the synthesis of new imidazolidine-4-one, thiazolidine-4-one, and oxazolidine-4-one derivatives derived from creatinine and to illustrate their influence on a colon cancer cell line and assess their antioxidant activity. Creatinine was reacted with α-chloroethyl acetate to produce 2-ethyl acetate creatinine 1. Then, the reaction of compound 1 with n-propyl bromide afforded N-propyl-2-ethylacetate creatinine 2. Compound 2 was then reacted with hydrazine hydrate to give hydrazide derivative 3. Schiff bases 4-6 were synthesized via the reaction of compound 3 with aromatic aldehydes (benzaldehyde and p-hydroxybenzaldehyde) and a ketone (p-amino acetophenone) in the presence of glacial acetic acid as a catalyst. Finally, Schiff bases 4-6 were treated with 2-aminoacetic acid to synthesize imidazolidine-4-one derivatives 7-9, with 2-thioglycolic acid to prepare thiazolidine-4-one derivatives 10-12, and with glycolic acid to synthesize oxazolidine-4-one derivatives 13-15. The newly synthesized compounds were identified using FT-IR and 1H NMR spectroscopy. In addition, the antioxidant and anticancer activities of some of the synthesized compounds were evaluated in vitro and showed good results.
2-hydrazinylbenzo[d]thiazole compound [1] is produced from reaction of 2-mercapto-benzothiazole with hydrazine hydride in ethanol. Compound [1] reacted with maleic anhydride in DMF to produce (Z)-4-(2-(benzo[d] thiazol-2yl) hydrazinyl)-4-oxobut-2-enoic acid [compound (2)]. While the treatment of compound [2] with the ammonium persulfate (NH4)2S2O8 (as the initiator) in order to produce compound [3], then compound [3] reacted with thionyl chloride in benzene to produce compound [4], finally compound [4] reaction with various drugs: cephalexin, amoxicillin, sulfamethizole, elecoxib obtained polymers [5–8]. The structure of synthesized compounds identified by spectral data: fourier transform infrared (FTIR) and proton nuclear magneti
... Show More2-hydrazinylbenzo[d]thiazole compound [1] is produced from reaction of 2-mercapto-benzothiazole with hydrazine hydride in ethanol. Compound [1] reacted with maleic anhydride in DMF to produce (Z)-4-(2-(benzo[d] thiazol-2yl) hydrazinyl)-4-oxobut-2-enoic acid [compound (2)]. While the treatment of compound [2] with the ammonium persulfate (NH4)2S2O8 (as the initiator) in order to produce compound [3], then compound [3] reacted with thionyl chloride in benzene to produce compound [4], finally compound [4] reaction with various drugs: cephalexin, amoxicillin, sulfamethizole, elecoxib obtained polymers [5–8]. The structure of synthesized compounds identified by spectral data: fourier transform infrared (FTIR) and proton nuclear magneti
... Show Moreتم تحضير ثلاث معقدات جديدة Ni (II)و Cu (II) و Zn (II) باستخدام الليكند المحضر الجديد من تفاعل حامض مالونيك ثنائي هيدرازايد مع 2-بيريدين كربوكسالديهايد. حيث شخصت المعقدات لمحضرة وكذلك الليكند باستخدام تقنيات مختلفة مثل FT-IR و UV-Vis و Mass و 1H-NMR و 13C-NMR وتحليل العناصر CHN و تقدير محتوى الكلور والموصلية المولارية والحساسية المغناطيسية والامتصاص الذري لتشخيص هذه المركبات. لكل معقد محضر جديد من النيكل والنحاس والزنك ، كشفت نتائج ا
... Show MoreSynthesis of 2-mercaptobenzothiazole (A1) is performed from the reaction of o-aminothiophenol and carbon disulfide CS2 in ethanol under basic condition. Compound (A1) is reacted with chloro acetyl chloride to give compound (A2). Hydrazide acid compound (A3) is obtained from the reaction of compound (A2) with hydrazine hydrate in ethanol under reflux in the presence of glacial acetic acid .The reaction of hydrazide acid compound (A3) with ethyl acetoacetate gives pyrazole compound (A4). The new hydrazone compound (A5) was prepared from the reaction of compound (A3) with benzaldehyde. Reaction of compound
... Show MoreSynthesis of new ligand, namely [bis(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl) hydrogen borate] (BIB), utilizing the reaction of metronidazole with boric acid in mole ratio (2:1), as well as the metal complexes with [Ni(II) and Cu(II)], were synthesized. All synthesized compounds were characterized by utilizing spectroscopic techniques such as FTIR, 1H-NMR, thermal analysis (T.G., UV-Vis), and atomic absorption (A.A.S.), as well as micro elemental analysis (C.H.N.), melting point (m.p), magnetic susceptibility, molar conductivity, and chloride content measurements. All complexes were paramagnetic, and the electrolyte and the suggested geometries were tetrahedral for nickel and octahedral for copper. In addition, all the transition meta
... Show MoreRecently, 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 da
... Show MoreA new ligand ( 4- methoxy benzoyl ) carbamothioyl ) Glycine (MCG) is synthesized by reaction of (4- methoxy benzoyl isothiocyanate) with Glycine(1:1). It is characterized by micro elemental analysis (C.H.N.S.), FT-IR, (UV-Vis) and 1H and 13CNMR spectra. Some metals ions complexes of this ligand were prepared and characterized byFT-IR,UV-Visible spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From results obtained, the following formula [M(MCG)2] where M2+ = Mn, Co, Ni, Cu, Zn, , Cd and Hg, the proposed molecular structure for these complexes as tetrahedral geometry, except copper complex is has square planer geometry.
Design and synthesis of novel poly heterocycles together using same heterocyclic compound is the main task of the present paper. The target compounds entitled 4,4’-[benzene-1,4-diylbis[ethylidenehydrazine-2-ylidene]bis[4-[3,5-di(5-substitutedpyridin-2-yl)-3,3a-dihydro[1,3]thiazolo[4,5-c][1,2]oxazol-6(5H)-yl]-4H-3-yl-1,2,4-triazole-3-thiol] have been synthesized starting from the reaction of 1,4-diacetylphenyl and carbohydrazide to give Schiff base derivatives then 1,2,4- triazole derivatives from the reaction with CS2 and an excess of hydrazine hydrate. The same applies for the condensing of these newly heterocyclic amines with different pyridine-2-carbaldehydes, which resulted in the synthesis of some new Schiff bases, whic
... Show MoreIn the present work, 9-fluorenone-2-carboxylic acid methyl ester (1) was prepared from 9-fluorenone-2-carboxylic acid and then converted into the acid hydrazide (2). Compound (2), is the key intermediate for the synthesis of several series of new compounds such as substituted 1,3,4-oxadiazole derivatives (3-6) were synthesized from the condensation of different substituted benzoic acids with compound (2) using POCl3 as condensing agent. Treatment of compound (2) with formic acid gave the N-formyl hydrazide (7), which upon refluxing with phosphorous pentoxide in benzene yielded the corresponding 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole (8). Reaction of hydrazide (2) with phenyl isocyanate to give N-phenyl semicarbazide derivative (9), then thi
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