Objective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the anticancer activities. Methods: Baclofen was initially reacted with aromatic aldehydes to create Schiff base derivatives (Ia–Ib), which were then closed in the next step using anhydrous acids to form oxazepine derivatives (IIa–IId). Results: The title compounds were synthesized successfully and identified using FT-IR, 1H NMR, and 13C NMR spectroscopy. Additionally, compound (IIc)’s (3-(4-chloro-phenyl)-4-[2-(4nitro-phenyl)-4,7-dioxo-4,7-dihydro-[1,3] oxazepin-3-yl]butyric acid) anticancer activity was assessed using MTT assay against FTC-133 (thyroid cancer) compared with WRL-68 (normal cell line). Discussion: The results showed that the viability of the FTC-133 cell was found to be greatest at 12.5 g/mL (96.52 ± 0.70) and lowest at 400 g/mL (35.378 ± 5.07). The effect of compound (IIc) on the normalizing of the WRL-68 cell line resulted in an IC50 for 62.39 ϻg/mL. Conclusions: It has been found that the compound (IIc) has good efficiency against thyroid cancer (FTC-133).
In this research, a group of complexes were prepared which were derived from Schiff base ligands, which is called (1E,1'E)-1,1'-(1,2-phenylene)bis(N-(2,4-dichlorophenyl) methanimine) (L) with ortho-phenanthroline (o-phen).The prepared complexes areM(II) [Co(II),Ni(II),Cu(II), Zn(II), Cd(II),and Hg(II)].A range of spectroscopic and technical techniques have been used to characterizethese materials, including:The FTIR, 1H-NMR, LC-Mass Spectrum, UV-Visbale, molar conductance, and magnaticmoment, atomic absorbtion, chlorid contents. Spectral results obtainedare showen that (ortho-phen) and (L) behave as neutral coordinating to the central metal ion by the donatingatoms(N2)of the both compounds. The geometry sha
... Show MoreAdvanced drug delivery systems offer undeniable benefits for drug delivery. In the past three decades, new methods have been proposed to develop a novel carriers for drug delivery. Nowadays, the major goal is to maximize therapeutic benefit while minimizing side effects. Drug delivery technique is clearly shifting from the micro to nanoscale. Nano-drug delivery systems (NDDSs) are the most promising approach utilized to improve the accuracy of drug delivery and the efficacy of drugs.In this narrative review article, we evaluate how delivery challenges associated with commercial marketed products and discuss newer DDS is being carried out to overcome these challenges .Different colloidal carrier systems such as carbon nanotube ,li
... Show MoreNew metal ions complexes of tridentate ligand (1-((dicyclohexylamino) methyl)-3-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrzol-4-ylimino) indolin-2-one) have been synthesized and characterized by chemical-physical analysis. The ligand acts as a tridentate for the complexation reaction with all metal ions. The new complexes, possessing the general formula [M(L)Cl]Cl where M=[Ni(II), Cu(II), Zn(II), Pd(II), Cd(II), Pt(IV) and Hg(II) ] ,show tetrahedral geometry. All complexes ,except Pd(II) complex which has a square planar geometry and Pt(IV) which show an octahedral geometry. The geometry of the prepared compounds has been proposed in another method theoretically by using one of the calculation molecular programs (Hype
... Show MoreThe complexes Shiff base and mixed ligands complexes of bipyridyl and Schiff base 1,5-dimethyl-4-(5-oxohexan-2-ylideneamino)-2-phenyl-1H-pyrazol-3(2H)-one (L) with Cr(III), Mn(II), Fe(II) and Co(II) were prepared. The compounds have been characterized by FT-IR, UV-Vis, mass and 1H and 13C-NMR spectra, magnetic moment, elemental microanalyses (C.H.N.), chloride containing, atomic absorption and molar conductance. The studies made are indicating towards octahedral geometry for these complexes. Hyper Chem-8 program has been used to prediction structural geometries of compounds in gas state, the heat of formation, binding energy, total energy and electronic energy and dipole moment at 298oK. The c
... Show MoreAmoxicillin 1 was treated with thiosemicarbazide and Phosphoryl chloride to obtain a new derivatives that contains 1,3,4-thiadiazole moiety 2. Schiff bases compounds were synthesized by the reaction of compound 2 with different aldehydes such as benzaldehyde and some substituted Benzaldehyde; p-hydroy, p-Chloro, p-Nitro, p-Dimethylamino, p-Methyl, p-Methoxy, p-Ethoxy to give compounds 3a-h. The obtained compounds have tested towards gram -ve and gram +ve bacteria. The compound shows good to moderate result towards the bacteria.
Schiff base derived from PVA and Erythroascorbic acid derivative (pentulosono-ɣ-lactone-2, 3-enedianisoate) was synthesized and characterized by Thin Layer Chromatography (TLC) and FTIR spectra, aldehyde was also characterized by (U.V-Vis), 1HNMR, 13CNMR and mass spectra. The inhibitory effect of prepared polymer on the activity of human serum Cholinesrerase has been studied in vitro. The polymer showed a remarkable activity at low concentration (4.5*10-3 – 4.5*10-8 M).
A new ligand complexes have been synthesis from reaction of metal ions of MnII , CoII , NiII , CuII , ZnII , CdII and PdII with schiff base [(E)-1-((2-amino-5-(3, 4, 5-trimethoxybenzyl) pyrimidin-4-ylimino) methyl) naphthalen-2-ol [HL)]. The prepared [HL] was characterized by FT-IR, UV-Vis spectroscopy, 1H13CNMR spectra Mass spectra and melting point. The compounds were characterized by techniques UV-Vis and FT-IR spectral studies, micro analysis (C.H.N), determination of atomic absorption, chloride content, molar conductivity measurements, magnetic susceptibility and melting point. The ligand acts as a monobasic tridentate, coordinating through deprotonated phenolic O and azomethine N atoms. The compounds are neutral electrolytic in dimeth
... 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 MoreTrimethoprim derivative Schiff bases are versatile ligands synthesized with carbonyl groups from the condensation of primary amines (amino acids). Because of their broad range of biological activity, these compounds are very important in the medical and pharmaceutical fields. Biological activities such as antibacterial, antifungal and antitumor activity are often seen. Transition metal complexes derived from biological activity Schiff base ligands have been commonly used.
Some new complexes of 4-(5-(1,5-dimethyl-3-oxo-2-phenyl pyrazolidin-4- ylimino)-3,3-dimethyl cyclohexylideneamino) -1,5- dimethyl-2- phenyl -1H- pyrazol -3(2H) –one (L) with Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Pd(II), Re(V) and Pt(IV) were prepared. The ligand and its metal complexes were characterized by phisco- chemical spectroscopic techniques. The spectral data were suggested that the (L) as a neutral tetradentate ligand is coordinated with the metal ions through two nitrogen and two oxygen atoms. These studies revealed Octahedral geometries for all metal complexes, except square planar for Pd(II) complex. Moreover, the thermodynamic activation parameters, such as ?E*, ?H, ?S, ?G and K are calculated from the TGA curves using Coa
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