Heterocyclic compounds are crucial for medicinal chemistry and the development of therapeutic agents like broad-spectrum antibiotics. This study devised a facile procedure to synthesize novel antimicrobial bicyclic heterocycles from 2-mercapto-3-phenylquinazolin-4(3H)-one. Advanced analytical techniques including 1 H and 13C NMR, elemental analysis, and FT-IR spectroscopy characterized the intricate chemical structures of the products. In vitro assays tested the heterocycles against aerobic and anaerobic bacterial strains using fluconazole and ciprofloxacin as antifungal and antibacterial controls. Results demonstrated the formidable broad-spectrum antibacterial and antifungal activities of the synthesized compounds, with growth inhibition approaching that of the positive controls. These findings highlight the immense potential of these novel heterocyclic compounds as antimicrobial agents. Further research can optimize their drug-like properties for eventual clinical use in combating drug-resistant infections.
Abstract
At any moment, the continuous usage of medications can accompanied by DNA damage and the accumulation of such damages can cause serious consequences. Antidepressants are long-term used drugs and the incidence of their genotoxic impacts cannot be excluded. Therefore, this work was designed to investigate the possible genotoxic effects of the commonly used antidepressants (fluoxetine and amitriptyline) in adult male rats.
Detection of DNA damage in individual cells was assessed by comet and micronucleus assays in three different cell populations i.e. liver, testis and bone marrow tissues of 24 swiss albino adult male rats. The animals were randomly allocated into three groups of 8 rats ea
... Show MoreCilnidipine is a dihydropyridine class of calcium channel blockers, it is classified as a BCS class II drug, characterized by a low oral bioavailability of 13%. Consequently, the utilization of nanoparticle preparation is anticipated to enhance its bioavailability. The objective of the research is to integrate cilnidipine nanoparticles into oral films as a means of enhancing patient adherence. The optimal polymers for producing Cilnidipine films were PVA cold and or HPMC E5 at different concentrations using a casting technique with glycerol as a plasticizer. The Nano suspension-based preparation of Cilnidipine's oral film containing the combination of polymers exhibited a significant enhancement in vitro dissolution, with a percentage excee
... Show MoreBackground This study aimed to evaluate the efficacy of once-daily liraglutide as an add-on to oral antidiabetics (OADs) on glycemic control and body weight in obese patients with inadequately controlled type 2 diabetes (T2D). Methods A total of 27 obese T2D patients who received 7 months (0.6 mg/day for the first month, 1.2 mg/day for 3 months, and 1.8 mg/day for 3 months) of liraglutide treatment as an add-on to OADs were included. Data on body weight (kg), fasting plasma glucose (FPG, mg/dL), postprandial glucose (PPG, mg/dL), and HbA1c (%), were recorded. Results Liraglutide doses of 1.2 mg/day and 1.8 mg/day were associated with significant decreases in body weight (by 8.0% and 11.9%, respectively, p < 0.01 for each) and HbA1c (by 20.0
... Show MoreIntroduction and Aim: Bacteriocins are antimicrobial peptides that have bactericidal and/or bacteriostatic activity against other bacteria. The aim of this study was to assess the antibacterial efficiency of Klebocin a K. pneumoniae bacteriocin, against biofilm formation by clinical isolates of methicillin resistant Staphylococcus aureus MRSA. Materials and Methods: S. aureus isolated from clinical samples was identified according to vitek 2 system Antibiotic susceptibility test was performed according to disc diffusion method. Vitek 2 compact system was also used to detect MRSA strains. Agar well diffusion method was used to evaluate the antibacterial activity of klebocin from K. pneumoniae towards 11 strains of S. aureus by
... Show MoreEleven yoghurt samples were collected from local markets in Baghdad to isolate Lactobacillus buchneri. Only 3 isolates of L. buchneri were found and the isolate No. 3 was the most producer of bacteriocin. Bacteriocin was adsorbed 100% onto silicic acid at pH 6.0-7.0. Below or above these pH values, adsorption was decreased, ranging between 35 and 90%. Therefore, pH 6.0 was used for the purification procedure. The purification procedure including silicic acid adsorption/desorption and cation-exchange chromatography (CEC) resulted in a 11.11 fold increase in the final specific activity of pure bacteriocin (1176.47 Au/mg) compared to the culture supernatant which was 32.64 Au/mg. The molecular weight was determined to be about 3.4 kDa. The bac
... Show MoreNimodipine (NMD) is a dihydropyridine calcium channel blocker useful for the prevention and treatment of delayed ischemic effects. It belongs to class ? drugs, which is characterized by low solubility and high permeability. This research aimed to prepare Nimodipine nanoparticles (NMD NPs) for the enhancement of solubility and dissolution rate. The formulation of nanoparticles was done by the solvent anti-solvent technique using either magnetic stirrer or bath sonicator for maintaining the motion of the antisolvent phase. Five different stabilizers were used to prepare NMD NPs( TPGS, Soluplus®, HPMC E5, PVP K90, and poloxamer 407). The selected formula F2, in which Soluplus
has been utilized as a stabilizer, has a par
... Show MoreI've been in this research preparation and diagnostic complexes mixed Kandat of Alcavaúan Alpiculan ion Althaaossianat with some metal ions has been reactive in ethanol solvent and distilled water by (1:1) and water complexes and lotions to the accounts of the metal in the complex
The aim of the present study is to formulate, evaluate and characterize the nanoemulsion of Domperidone a poorly water-soluble anti-emetic drug.
Domperidone powder is white or almost white powder, photosensitive, practically insoluble in water, slightly soluble in ethanol and in methanol; soluble in dimethylformamide. It is used as an antiemetic for the short-term treatment of nausea and vomiting of various etiologies.
Solubility studies were conducted to select the oil, surfactant and cosurfactant. Phase diagrams were constructed by aqueous phase
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