Microwave irradiations toprepare novel 1,4-dihydropyridine, pyrimidoquinoline, triazoloquinazolinone,and imidazoquinazolinonedimer analogsand their antimicrobial performances

IF 4.1 3区 化学 Q2 CHEMISTRY, PHYSICAL
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Abstract

The main intentof this work is to create novel 1,4-dihydropyridine, pyrimidoquinoline, triazoloquinazolinone, and imidazoquinazolinone dimers through microwave irradiation. These conformers were then evaluated for their capacity to impede the spread of bacteria in vitro against Salmonella typhi, Listeria monocytogenes, Candida albicans, Escherichia coli, and Staphylococcus aureus. The effective positive control substances involved vancomycin and ampicillin.With a MIC level between 57 to 147 mg/mL, substrates 3, 5, 7a, 7b, 9, and 12 shown the modest effectiveness towards inhibiting the growth both of bacteria and fungi. Compounds 13, 19, 15a, 15b, and 17 demonstrated excellent effectiveness in inhibiting the growth of the candida albicans fungus, with MIC level between 51 to 74 mg/mL, matching the positive control.With MIC level between 62 to 82 mg/mL, analogs 13, 19, 15a, and 15b showed outstanding activity against four different bacterial strains for growth suppression. Their activity was comparable to that of the positive control. Furthermore, compound 17 demonstrates remarkable growth inhibitory activity, outperforming the positive control in the 69–86 mg/mL MIC range. The dimer derivative triazoloquinazolinone 17 showed excellent antibacterial efficacy and showed tremendous promise for development into medicinal drugs in the future.

这项工作的主要目的是通过微波辐照制造新型 1,4-二氢吡啶、嘧啶并喹啉、三唑并喹唑啉酮和咪唑并喹唑啉酮二聚体。然后评估了这些构象物对伤寒沙门氏菌、单核细胞增生李斯特菌、白色念珠菌、大肠杆菌和金黄色葡萄球菌的体外抑制细菌扩散的能力。底物 3、5、7a、7b、9 和 12 的 MIC 值介于 57 至 147 毫克/毫升之间,对抑制细菌和真菌的生长具有一定的效果。化合物 13、19、15a、15b 和 17 在抑制白色念珠菌真菌生长方面表现出卓越的功效,其 MIC 值介于 51 至 74 毫克/毫升之间,与阳性对照相匹配。类似物 13、19、15a 和 15b 的 MIC 值介于 62 至 82 毫克/毫升之间,在抑制四种不同细菌菌株的生长方面表现出卓越的活性。它们的活性与阳性对照相当。此外,化合物 17 显示出显著的生长抑制活性,在 69-86 毫克/毫升的 MIC 范围内优于阳性对照。三唑并喹唑啉酮 17 的二聚体衍生物显示出卓越的抗菌功效,未来有望开发成药物。
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来源期刊
CiteScore
7.90
自引率
7.00%
发文量
580
审稿时长
48 days
期刊介绍: JPPA publishes the results of fundamental studies on all aspects of chemical phenomena induced by interactions between light and molecules/matter of all kinds. All systems capable of being described at the molecular or integrated multimolecular level are appropriate for the journal. This includes all molecular chemical species as well as biomolecular, supramolecular, polymer and other macromolecular systems, as well as solid state photochemistry. In addition, the journal publishes studies of semiconductor and other photoactive organic and inorganic materials, photocatalysis (organic, inorganic, supramolecular and superconductor). The scope includes condensed and gas phase photochemistry, as well as synchrotron radiation chemistry. A broad range of processes and techniques in photochemistry are covered such as light induced energy, electron and proton transfer; nonlinear photochemical behavior; mechanistic investigation of photochemical reactions and identification of the products of photochemical reactions; quantum yield determinations and measurements of rate constants for primary and secondary photochemical processes; steady-state and time-resolved emission, ultrafast spectroscopic methods, single molecule spectroscopy, time resolved X-ray diffraction, luminescence microscopy, and scattering spectroscopy applied to photochemistry. Papers in emerging and applied areas such as luminescent sensors, electroluminescence, solar energy conversion, atmospheric photochemistry, environmental remediation, and related photocatalytic chemistry are also welcome.
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