A new series of schiff base and aminothiadiazole derivatives of N- substituted phthalimide (I-VI) were synthesized. In this work, the intermediate 4-(1,3-dioxoisoindolin-2-yl)benzaldehyde compound (I), was formed by reaction of 4-amino benzaldehyde with phthalic anhydride in glacial acetic acid(GAA). A series of Schiff bases (IV-VI) was prepared by the reaction of benzidine with compound (I) in ethanol and presence of GAA as a catalyst to form compound (IV) which react with compound (I) and p-nitro benzyldehyde to give compound (V) and (VI) respectively. A new phthalimide thiosemi-carbazone derivative (ll) was prepared by reaction of compound (l) with thiosemi-carbazide HCl in the presence of equimolar amount of sodium acetate. Finally, a new phthalimide containing (1,3,4- thiadiazole ring) compound (III) was formed by bromine mediated “oxidative intramolecular cyclization” of compound (I) in the presence of sodium acetate. All of the final target compounds' structures were successfully synthesized and confirmed using analytical and spectroscopic data. These compounds were identified and confirmed by melting points, TLC, FT IR, and 1H NMR. While the antimicrobial effect of the new derivatives has been assessed in vitro against G-positive, G-negative bacteria and fungi activity. All screened compounds exhibited no activity against G-positive bacteria (Staph. Aureus, and Bacillus subtilis). Many of synthesized compounds displayed moderate effect against “G-negative bacteria Escherichia coli, and Klebsiella pneumonia and against Candida tropicalis”. While the best antifungal activity was obtained from compound I which has high activity against Candida tropicalis.
Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory resu
... Show More1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.
To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.
The designed compounds were synthesized using convent
The organic compound imidazole has the chemical formula C3N2H4. Numerous significant biological compounds contain imidazole. The amino acid histidine is the most prevalent. The substituted imidazole derivatives have great potential for treating a variety of systemic fungi infections. Thiourea is an organosulfur compound with the formula SC(NH2)2. It is a reagent in organic synthesis. In this paper, some new imidazole and thiourea derivatives are synthesized, characterized, and studied for their biological activity. These new compounds were synthesized from the starting material terephthalic acid, which was transformed to corresponding ester [I] by the refluxing of diacid with methanol in the presence of H2SO4 as a catalyst, compound [I] con
... Show MoreA new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compound
... Show MoreA new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compound
... Show More(E)-2-(benzo[d]thiazol-2-yliazenyl)-4-methoxyaniline was synthesized by reaction the diazonium salt of 2-aminobenzothiazole with 4-methoxyaniline. Identified of the ligand by spectral techniques (UV-Vis, FTIR,1HNMR and LC-Mass) and microelemental analysis (C.H.N.S.O) are used to produce of the azo ligand. Complexes of (Co2+, Ni2+, Cu2+ and Zn2+) were synthesized and identified using atomic absorption of flame, elemental analysis, infrared and UV-Vis spectral process as well conductivity and magnetic quantifications. Nature of compounds produced have been studied followed the mole ratio and continuous contrast methods, Beer's law followed during a concentration scope (1×10-4-3×10-4 mole/L). height molar absorptivity of compound solutions h
... Show MoreA series of overbased magnesium fatty acids such as caprylate, caprate, laurate, myristate, palmitate, stearate and oleate) were synthesized by the reaction of the fatty acids with active – 60 magnesium oxide and carbon dioxide (CO2) gas at 60 oC in the presence of ammonia solution as catalyst, toluene / ethanol solvent mixture (9:1vol/vol) was added.
The prepared detergent additives were characterized by FTIR, 1HNMR and evaluated by blending each additive in various concentrations with medium lubricant oil fraction (60 stock) supplied by Iraqi Midland Refineries Company. The total base number (TBN, mg of KOH/g) was determined, and the results of TBN were treated by using two-way analysis of variance (ANOVA) test. It was found that
In recent years , the interest in gold (III) species have gained more and more attention for cancer chemotherapy , this was stimulating by the possibility to develop new agents with mode of action and clinical profile different from the established platinum metalodrugs.
With this frame, recently new square planar Au(III) complexes (Au(L)(L')n); where L=SCH2COO- ; L'=HSCH2COO- had been synthesized with S/O – donor ligands.
In this article and by the aim to replace, one of (L') ligand by anion chloride ligand (which supposedly more relevant for the biodistribution of the compound than for its pharmacodynamic effects), new complex (Au(L')
A new ligand N-((4-(phenylamino) phenyl) carbamothioyl) acetamide (PCA) was synthesized by reaction of (4-amino di phenyl amine) with (acetyl isothiocyante) by using acetone as a solvent. The prepared ligand(PCA) has been characterization by elemental analysis (CHNS), infrared(FT-IR),electronic spectral (UV-Vis)&1H,13C- NMR spectra. Some Divalent Metal ion complexes of ligand (PCA) were prepared and spectroscopic studies by infrared(FT-IR), electronic spectral (UV-Vis), molar conductance, magnetic susceptibility and atomic absorption. The results measured showed the formula ofFall prepared complexes were [M (PCA)2 Cl2] (M+2 = Mn, Co, Ni, CU, Zn, Cd &Hg),the proposed geometrical structure for all complexes wereeoctahedral.