Objective:This study involved synthesis of a new series of different five-membered heterocyclic derivatives, testing their antioxidant activity, and examining their potential in vitro antimicrobial agents. Methods: The synthesis of the derivatives involved a three-step process. Initially, succinyl chloride was reacted with methanol, followed by a reaction with 80% hydrazine hydrate through a nucleophilic addition-elimination mechanism, resulting in the formation of succinohydrazide (I). This compound was then employed as a precursor for the synthesis of Schiff bases (II), and (III) by reacting it with m-nitro benzaldehyde and p-nitro benzaldehyde. Following this, a ring closure reaction was applied using thioglycolic acid, glycolic acid, and glycine, resulting in the synthesis of different five-membered heterocyclic rings (IV–IX). Results and Discussion: The formation of the prepared derivatives was confirmed by FT-IR, 1H NMR, and 13C NMR spectroscopy. Comparative analysis with L-ascorbic acid as a standard revealed that all the prepared compounds exhibited excellent antioxidant activities. In terms of antimicrobial activity, the tested derivatives showed moderate activity against both positive and negative types of bacteria, when compared to the reference drug Ciprofloxacin. Additionally, the antifungal test showed moderate activity for all the tested compounds against a specific pathogenic fungus, with Clotrimazole being as the reference drug. The antimicrobial activity of the synthesized compounds was found to be dependent on the type of heterocyclic rings containing S, O, and N atoms. These atoms were observed to enhance antimicrobial activity by donating electrons and becoming active. Additionally, the presence of active functional groups such as C=O, NO2, and C=N contributed to this observed result. Conclusions: All of the synthesized compounds have demonstrated excellent antioxidant agents. Most of them have shown promising antimicrobial activity against certain bacteria strains, and effectiveness against a pathogenic fungus.
A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of di
... Show MoreAcinetobacter baumannii (A. baumannii) is a major opportunistic nosocomial pathogen, mostly resistant to several groups of antibiotics. Colistin is now used as a last-line treatment for isolates that are highly resistant. The purpose of this study is to identify the importance of LptD; which is involved in the translocation of LPS from the inner membrane to the outer membrane in compartment with LptA and LptC of A. baumannii and its indispensable role as a virulence factor, and the efficiency of colistin as a monotherapy. In the current research, two isolates of A.baumannii were used, the local isolate HHR1 isolated from urine sample and the global strain ATCC 17904, and three antibiot
... Show MoreFelodipine is a calcium-channel blocker with low aqueous solubility and bioavailability. Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE) is one of the popular methods that has been used to solve the dispersibility problems of many drugs. Felodipine was formulated as a NE utilizing oleic acid as an oil phase, tween 80 and tween 60 as surfactants and ethanol as a co-surfactant. Eight formulas were prepared, and different tests were performed to ensure the stability of the NEs, such as particle size, polydispersity index, zeta potential, dilution test, drug content, viscosity and in-vitro drug release. Result
... Show MoreBackground and Aim: The use of food dyes can cause certain diseases, such as anemia and indigestion, along with other disorders, tumors, and even cancer. Therefore, this study aimed to determine the chemical nature and toxicity of some commercial dyes locally used in processed foods compared with standard food dyes. Materials and Methods: Three types of standard and commercial food color additives (Sunset Yellow, Tartrazine, and Carmoisine) were extensively examined. The chemical structures and functional groups of the dyes were evaluated by Fourier-transform infrared (FTIR) spectroscopy. The melting temperatures of the dyes were also determined by chemical thermal analysis. The acute toxicity test to evaluate the standard and commercial
... Show MoreThe research includes synthesis and identification of novel three amino acids ligands complexes of some heavy metal (II) ions by using the amino acids like glycine, L-alanine and L-valine. New metal mixed ligand complexes with amino acids are prepared the reaction by reacting the three amino acids with the metals(II) chloride by using 50% ethanolic solution and 50% distall water in the molar ratio [1:1:1:1] ( M:Gly:Ala:Val) except for Co(II) and Ni(II) complexes were found after diagnosis the coordination with both Lalanine and L-valine. The prepared complexes identified by using physical properties, flame atomic absorption and conductivity measurements, in addition, mass, FT.IR and UV.vis spectrum as well magnetic moment data. The general
... Show MoreObjective(s): Biocompatibility, non-toxicity, minimal allergenicity, and biodegradability are all characteristics of chitosan. Other biological properties of chitosan have been reported, including antitumor, antimicrobial and antioxidant activities. This research aim is the synthesis of drug compounds by preparation and characterization of polymer chitosan Schiff base and chitosan Schiff base / Poly vinyl alcohol / poly vinyl pyrrolidone Nanocomposite and study applications (anticancer cell line, antimicrobial agents). Methods: Chitosan Schiff base was prepared from the reaction of chitosan with carbonyl group of 4-nitro benzaldehyde. Polymer blend have been prepared by solution casting method. Chitosan Schiff base mixing with PVA and PVP
... Show Morein this work the polymides were prepared as rthemally stable polymers by diffrent ways
A series of Schiff base-bearing salicylaldehyde moiety compounds (1-4) had been designed, synthesized, subjected to insilico ADMET prediction, molecular docking, characterization by FT-IR, and CHNS analysis techniques, and finally to their Anti-inflammatory profile using cyclooxygenase fluorescence inhibitor screening assay methods along with standard drugs, celecoxib, and diclofenac. The ADMET studies were used to predict which compounds would be suitable for oral administration, as well as absorption sites, bioavailability, TPSA, and drug likeness. According to the results of ADME data, all of the produced chemicals can be absorbed through the GIT and have passed Lipinski’s rule of five. Through molecular docking with PyRx 0.8, these
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