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 total of 200 samples (180 fecal materials and 20 organ samples) were collected from (5 different poultry farms, 10 local poultry shops, 5 houses poultry, 5 Eggs stores shops and 5hand slaughters centers) in Ibb city, Yemen, 2014. According to morphological, cultural, as well as biochemical characterization and serological tests, 59(29.5%) isolates were identified as Salmonella spp. and all Salmonella isolates were categorized by serotype, which comprised of, 37(62.71%) Salmonella Typhimurium serovar, 21(35.59%). Salmonella Enteritidis serovar and 1(1.69%) Salmonella Heidlberg serovar. Antibiotic sensitivity test was done for bacterial isolates and the results showed there were clear differences in antibiotic resistant. Antimicrobial
... Show MoreSelexipag is an orally selective long-acting prostacyclin receptor agonist, which indicated for the treatment of pulmonary arterial hypertension. It is practically insoluble in water ( class II, according to BCS). This work aims to prepare and optimized Selexipag nanosuspensions to achieve an enhancement in the in vitro dissolution rate. The solvent antisolvent precipitation method was used for the production of nanosuspension, and the effect of formulation parameters (stabilizer type, drug: stabilizer ratio, and use of co-stabilizer) and process parameter (stirring speed) on the particle size and polydispersity index were studied. SLPNS prepared with Soluplus® as amain stabilizer (F15) showed the smallest particle size 47nm wi
... Show MorePatch in transdermal drug delivery(TDDS) used to overcome the hypodermic drawback, but these patch also have absorption limitation for hydrophilic and macromolecule like peptide and DNA. So that micronized projection have the ability for skin penetration developed named as microneedle. Microneedle drug delivery system is a novel drug delivery to overcome the limitation of TDDS like skin barrier restriction for large molecule. Microneedle patch can penetrate through skin subcutaneous into epidermis, avoiding nerve fiber and blood vessel contact. There are many type of microneedle patch like solid, polymer, hallow, hydrogel forming microneedle and dissolving microneedle with different method of microfabrication
Cubosomes are nanosized structures self-assembled nanostructured materials used for controlling the release of the entrapped drug molecule. Lornoxicam (LXM) is a potent analgesic nonsteroidal anti-inflammatory (NSAID) drug with a short half-life (3-4) hours. The present study aims to prepare LXM-loaded cubosomes with well-defined morphology, particle size, PDI, high entrapment efficiency, sustained drug release, and high zeta potential value, as a transdermal drug delivery system.
Twelve formulas of LXM-loaded cubosomal dispersions were prepared by a solvent dilution method using Glyceryl monooleate ( GMO) as polar lipid with different stabilizers as Pluronic® F127 or tween 80 and different types o
... Show MoreUnregulated epigenetic modifications, including histone acetylation/deacetylation mediated by histone acetyltransferases (HATs) and histone deacetylases (HDACs), contribute to cancer progression. HDACs, often overexpressed in cancer, downregulate tumor suppressor genes, making them crucial targets for treatment. This work aimed to develop non‐hydroxamate benzoic acid–based HDAC inhibitors (HDACi) with comparable effect to the currently four FDA‐approved HDACi, which are known for their poor solubility, poor distribution, and significant side effects. All compounds were structurally verified using FTIR, 1HNMR, 13CNMR, and mass spectrometry. In silico ana
Background: Reduction in bond strength when bonding was done immediately after intracoronal bleaching procedure has been recognized. The purpose of this study is to assess the effect of antioxidants (10% sodium ascorbate (SA), 0.1M thiourea and7% sodium bicarbonate (SB)) on reversing bonding strength of composite resin to bleached dentin. Materials and method: Sixty upper 1st premolar teeth, were selected, the crowns of the teeth were embedded in acrylic resin blocks exposing a flat dentin from the buccal surface, then divided into 6 groups (10 samples each). Bleaching for the experimental groups was performed using 35% hydrogen peroxide bleaching gel (pola–office).Group A (Negative
... Show MoreA new hetrocyclic liquid crystal compounds containing 1,3,4-oxadiazole with different substituted in para position (Bromo, Chloro, Nitro and Methyl) were synthesized and characterized by melting points, FTIR Spectroscopy and 1HNMR spectroscopy for [Cl-SR6] and [NO2-SR6] compounds. The liquid crystalline properties of the synthesized compounds were studied by using hot-stage polarizing optical microscopy (POM), so they determined the transition enthalpies and entropies by using differential scanning calorimetery (DSC). All of the compounds show mesomorphic properties. The compounds [Br-SR6], [Cl-SR6] and [NO2SR6] exhibit an enantiotropic dimorphism smectic (Sm) phase, while the compounds [MeSR6] showed nematic (N) phase throw cooli
... Show MoreThe work includes synthesis and characterization of some new heterocyclic compounds, as flow: The compound (3) (5-(4-chlorophenyl) -2-hydrazinyl-1,3,4-oxadiazole was synthesized by using two methods; the first method includes the direct reaction between hydrazine hydrate 80% and 5-(4-chlorophenyl)-2- (ethylthio) 1,3,4-oxadiazole (1), the second method involves converting 5-(4-chlorophenyl)-1,3,4-oxadiazol-2-amine (2) to diazonium salt then reducing this salt to compound (3) by stannous chloride. Compound (3) was used as starting material for synthesizing several fused heterocyclic compounds. The compound 6-(4- chlorophenyl)[1,2.4] triazolo [3,4,b][1,3,4] oxadiazole-3-(2H) thione (compound 4) was synthesized from the reaction of compo
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