The design of novel materials with significant biological properties is a main target in drug design research. Chromene compounds represent an interesting medicinal scaffold in drug replacement ...systems. This report illustrates a successful synthesis and characterization of two novel series of
compounds using multi-component reactions. The synthesis of the first example of azo chromophores containing chromene moieties has also been established using the same methodology. The antimicrobial activity of the new molecules has been tested against seven human pathogens including two Gm+ve, two Gm-ve bacteria, and four fungi, and the results of the inhibition zones with minimum inhibitory concentrations were reported as compared to reference drugs. All the designed compounds showed significant potent antimicrobial activities, among of them, four potent compounds
,
,
, and
showed promising MIC from 0.007 to 3.9 µg/mL. In addition, antiproliferative analysis against three target cell lines was examined for the novel compounds. Compounds
,
,
, and
possessed significant antiproliferative activity against three cell lines with an IC
of 0.3 to 2 µg/mL. Apoptotic analysis was performed for the most potent compounds via caspase enzyme activity assays as a potential mechanism for their antiproliferative effects. Finally, the computational 2D QSAR and docking simulations were accomplished for structure-activity relationship analyses.
Objective: The aim of the method was to develop a novel, simple and rapid fluorometric method determination of Amiloride (AMD) in pure form and pharmaceutical drugs via fluorescence measurements.
...Methods: The method depends on fluorescence quenching of 2H-chromene azo dye (2-(4-nitrophenyl)-N-(4-(phenyldiazenyl)-2H-chromen-4-amine) upon adding Amiloride (AMD) using homemade ISNAG 2 X 90° multi solar cell via low-pressure mercury lamp at two significant wavelengths 184.9 and 253.7 nm combined with continuous flow injection analysis.
Results: Under the optimized conditions, the fluorescence quenching linear working range and percentage linearity (r2%) was (0.03-8 mmol/l) and 98.78 %, respectively. The suggested method was effectively applied to the determination of AMD in two different pharmaceutical drugs and compared with the classical method (UV-vis spectrophotometry at λ=540 nm).
Conclusion: The proposed and established method is simple, direct, and efficient. The statistical comparison results using a t-test at 95% confidence interval that was applied to compare the new and classical method showed there are no significant differences between the two methods.
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