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.
The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon).
Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting
This study aimed for isolation and identification of Candida glabrata and identifying some virulence factors. The distribution of patients with candidemia thrush showed that the age group 50-65 years old recorded the highest incidence of candidiasis in female and male with leukemia by 50% and 37.9 % respectively compared to the lowest incidence of candidiasis in the age group under 17 years old in female and male 8.8% and 13.5%, respectively. While the age group between 5-8 years was high, reaching 18 cases of oral candidiasis and 42% of children with leukemia compared with the age group, which was the least, that reached 9 cases, 21%. The highest incidence of C. glabrata was 59 isolates of females and males with leukemia, while C. kefyer w
... Show MoreThe synthesis and structural characterization of new dithiocarbamate (DTC) ligand and some of its dinuclear transition metal complexes are described. The free dithiocarbamate ligand was prepared through several synthetic routes, including Schiff-base formation. The reaction of 2-aminopropane with terephthaldehyde leads to the formation of Schiff_base which is reduced by methanolic NaBH4 to the corresponding secondary diamine. Diamine( N,N'_ (1,4 phenylenebis (methylene)) bis(propan-2 amine)) reacts with (CS2) in a basic solution of (KOH) to provide the corresponding bis(dithiocarbamate) free_ligand, which undergoes complexation with the appropriate metal (II) chlori
... Show MoreBackground: The elimination of the microorganisms from the root canal systems, an important step for the successful root canal treatment. This study was conducted to evaluate the antibacterial effectiveness of the photoactivated disinfection by using the toluidine blue O and a low- energy light emitting diode (LED) lamp . Materials and method: Sixty single rooted extracted teeth were decoronated, instrumented, irrigated, sealed at the apex and contaminated with endodontic anaerobic bacteria for 7 days to form biofilms in prepared root canals. Group I. Twelve teeth were medicated by photosensitizer (toluidine blue O) solution activated by diode lamp (FotoSan; CMS Dental, Copenhagen, Denmark).Group II. Twelve teeth were medicated by the tricr
... Show MoreLeishmaniasis is a disease caused by a protozoan parasite of the genus Leishmania. It is transmitted by the bite of sandfly (Subfamily Phlebotominae). Limited drugs are available for the treatment of leishmaniasis, and the general drug (pentostam) have many side effect on patients. Therefore, there is an urgent need for another drugs for the treatment of leishmaniasis.
This study aimed to develop new type of antileishmanial agents instead of classical drug (pentostam) and investigated the effectiveness of silver nanoparticles (Ag NPs) on Leishmania tropica parasites in both phases promastigote and amastigote in comparision to pentostam in in vitro condition.
This study showed the effects of Ag NPs in comparision to pentostam with d
Four photosensitizers were used to test inhibitory effect of Helicobacter pylori bacteria using
low power helium: neon red laser radiation. Biopsies were collected from 176 patients and H. pylori were
isolated, identified and bacterial suspension was prepared. Samples of this suspension were mixed with
various low concentrations of the test sensitizer. The mixture samples were exposed to different laser
radiation doses. The samples were then inoculated and the inhibition zones were studied and compared
with their analogues of control samples. The most effective sensitizer with optimum concentration and
irradiation dose was determined. Statistical analysis of results was performed. The sensitizers' toluidine
blue and
In this research, the preparation of bidentate Schiff base was carried out via the condensation reaction of both the salicylaldehyde with 1-phenyl-2,3-dimethyl-4-amino-5-oxo-pyrazole to form the ligand (L). The mentioned ligand was used to prepare complexes with transition metal ions Mn(II), Co(II), Ni(II), Cu(II) and Zn(II). The resulting complexes were separated and characterized by FTIR and UV-Vis spectroscopic technique. Elemental analysis for Carbon, Hydrogen and Nitrogen elements, electronic spectra of the ligand and complexes were obtained, and the magnetic susceptibility tests were also achieved to measure the dipole moments. The molar conductivities were also measured and determination of chlorine content in the complexes and
... Show MoreBackground: The present study was conducted to evaluate the effects of different bleaching methods on the shear bond strength of orthodontic Sapphire brackets bonded to human premolars teeth using light cured composite resin and to determine the predominant site of bond failure. Materials and Methods: Thirty freshly extracted human premolars were selected and randomly divided into three groups (10 per group). These groups are: control (unbleached) group, hydrogen peroxide group (HP) 37.5% ; which is the in- office bleaching method group, carbamide peroxide group (CP) 16%; which is the at- home bleaching method group. After bleaching process was performed, all the teeth stored in distilled water in a sealed container at room temperature for
... Show MoreTwo isolates of Pseudomonas aeruginosa were isolated from patients with Urinary Tract Infection (UTI). The aim of this study was to determine the antimicrobial effect of alcoholic leaves extract of Salvia officinalis on Multidrug resistant (MDR) P. aeruginosa. Using the well diffusion test, the alcoholic leaves extract at 100mg/ml and 200 mg /ml was shown to possess antimicrobial activity against the tested microorganism. The inhibition zones of S. officinalis at 200 mg/ml, and 100 mg/ml of the extract showed diameters of 23mm and 20mm, respectively. But the diameters of the inhibition zones caused by treatment with the antibiotics Ciprofloxacin, Ticarcillin + Clavulanic acid, and Cefotaxime w
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