10 research outputs found
Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles
No full textUltrasound-assisted synthesis of novel 1,2,3-triazoles coupled diaryl sulfone moieties by the CuAAC reaction, and biological evaluation of them as antioxidant and antimicrobial agents
Get PDFA series of 1,2,3-triazoles coupled diaryl sulfone containing compounds were synthesized by the copper-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC) reaction in benign solvents under ultrasound irradiation. In situ formation of azides from α-bromoketones together with the CuAAC reaction in one pot allowed safe handling and good availability of azides for the development of a small library of compounds. The sonication reduced reaction time and increased yields compared to otherwise same conditions. All synthesized compounds were evaluated for antibacterial, antifungal and antioxidant activities. Compounds 3b, 6b and 9e–9g were found to be the most potent antifungal agents with minimal inhibitory concentration (MIC) at 25 μg/mL; moreover other compounds revealed good to moderate antimicrobial activity. Compound 8e showed an excellent antioxidant activity using a DPPH free radical scavenging assay
Improved vaginal retention and enhanced antifungal activity of miconazole microsponges gel: Formulation development and in vivo therapeutic efficacy in rats
No full textDevelopment of Promising Thiopyrimidine-Based Anti-cancer and Antimicrobial Agents: Synthesis and QSAR Analysis
No full text
Objective & Methodology:
New hybrids of thiopyrimidine-five/six heterocyclic rings were
synthesized and in vitro evaluated for their antiproliferative activity against three human cancer cell
lines, namely HCT116 (human colorectal carcinoma), PC-3 (human prostate adenocarcinoma) and
HepG2 (human liver carcinoma) cell lines. The most potency was elicited by the target candidates
against the viability of HCT116 cell lines. It was higher than that obtained by the positive control
5-Fluorouracil (IC50 range; 0.11-0.49 μM, IC50, 5-FU; 1.10 μM).
Results:
Cell cycle analysis and apoptosis activation revealed that compound 20 induced G2/M phase
arrest and apoptosis in HCT116 cells. In addition, compound 20 activates the caspases-9 and -3, a
process which might mediate the apoptosis of HCT116 cells.
Conclusion:
Furthermore, there is a good agreement between the observed pIC50 and the predicted
pIC50 values, in addition, the low RMSD and standard error values indicate the accuracy of the model.
Antimicrobial evaluation revealed that some of these compounds exhibited significant activities
against the tested pathogenic bacteria and fungi, wherein compounds 7a, 14, 15a, 21a, produced the
most potent and broad spectrum antibacterial and antifungal potency that was equivalent to that revealed
by Vibramycin and Ketoconazole (MIC; 125 μg/mL). Moreover, compounds 15a, 21c, investigated
dual potent antimicrobial and anticancer activity.
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Chitosan/sulfobutylether-β-cyclodextrin nanoparticles as a potential approach for ocular drug delivery
No full textNovel 1,2,3-Triazole Derivatives as Antimicrobial Agents
No full text2-Substituted benzimidazoles 3a-c was prepared via condensation of ethyl pyruvates 2a-c with 2-phenylenediamine in glacial acetic acid. Pyrrolo[1,2-a]benzimidazole derivatives 5 and 8 were prepared via cyclocondensation of compounds 3a,b with phosphorus oxychloride or acetic anhydride in presence of sodium acetate respectively. Reactivity of pyruvate 2 towards 2-aminophenol, hydroxylamine and cyanothioacetamide was also investigated. They exhibited potent antimicrobial activity comparable to clinical drugs such as ciprofloxacin and ketoconazole. Compounds 3a, 11 and 13 showed excellent antimicrobial activity against all the tested microbes, and Compound 11 showed lower MIC values against all the tested organisms
Optimization of pectinase immobilization on grafted alginate-agar gel beads by 24 full factorial CCD and thermodynamic profiling for evaluating of operational covalent immobilization
No full textOptimization of Enterococcus faecalis Esawy KR758759 dextransucrase and evaluation of some dextran bioactivities
No full textSynthesis and Evaluation of New Coumarin Derivatives as Antioxidant, Antimicrobial, and Anti-Inflammatory Agents
No full textNew pyranocoumarin and coumarin-sulfonamide derivatives were prepared and evaluated for their antioxidant, antimicrobial, and/or anti-inflammatory activities. Coumarin-sulfonamide compounds 8a–d demonstrated significant antioxidant activity, while 7c,d, 8c,d, and 9c,d exhibited antimicrobial activity equal to or higher than the standard antimicrobials against at least one tested microorganism. Regarding the anti-inflammatory testing, pyranocoumarins 2b, 3a,b and 5c and coumarin-sulfonamide compound 9a showed more potent antiproteinase activity than aspirin in vitro; however, five compounds were as potent as aspirin. The anti-inflammatory activity of the promising compounds was further assessed pharmacologically on formaldehyde-induced rat paw oedema and showed significant inhibition of oedema. For in vitro COX-inhibitory activity of coumarin derivatives, pyranocoumarin derivative 5a was the most selective (SI = 152) and coumarin-sulfonamide derivative 8d was most active toward COX-2 isozyme. The most active derivatives met the in silico criteria for orally active drugs; thus, they may serve as promising candidates to develop more potent and highly efficient antioxidant, antimicrobial, and/or anti-inflammatory agents
