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新型 2-硫代海因和 2-喹诺酮衍生物的蓝光激活杂合抗菌活性的初步研究。

Preliminary Studies of Antimicrobial Activity of New Synthesized Hybrids of 2-Thiohydantoin and 2-Quinolone Derivatives Activated with Blue Light.

机构信息

Institute of Biology, Pedagogical University of Krakow, Podchorążych 2, 30-084 Kraków, Poland.

Department of Biophysics, Faculty of Biochemistry, Biophysics and Biotechnology, Jagiellonian University, Gronostajowa 7, 30-387 Kraków, Poland.

出版信息

Molecules. 2022 Feb 5;27(3):1069. doi: 10.3390/molecules27031069.

Abstract

Thiohydantoin and quinolone derivatives have attracted researchers' attention because of a broad spectrum of their medical applications. The aim of our research was to synthesize and analyze the antimicrobial properties of novel 2-thiohydantoin and 2-quinolone derivatives. For this purpose, two series of hybrid compounds were synthesized. Both series consisted of 2-thiohydantoin core and 2-quinolone derivative ring, however one of them was enriched with an acetic acid group at N3 atom in 2-thiohydantoin core. Antibacterial properties of these compounds were examined against bacteria: , , , , , and . The antimicrobial assay was carried out using a serial dilution method to obtain the MIC. The influence of blue light irradiation on the tested compounds was investigated. The relative yield of singlet oxygen (O*, Δ) generation upon excitation with 420 nm was determined by a comparative method, employing perinaphthenone (PN) as a standard. Antimicrobial properties were also investigated after blue light irradiation of the suspensions of the hybrids and bacteria placed in microtitrate plates. Preliminary results confirmed that some of the hybrid compounds showed bacteriostatic activity to the reference Gram-positive bacterial strains and a few of them were bacteriostatic towards Gram-negative bacteria, as well. Blue light activation enhanced bacteriostatic effect of the tested compounds.

摘要

硫代海因和喹诺酮衍生物因其广泛的医疗应用而引起了研究人员的关注。我们的研究目的是合成和分析新型 2-硫代海因和 2-喹诺酮衍生物的抗菌性能。为此,合成了两个系列的混合化合物。这两个系列都由 2-硫代海因核心和 2-喹诺酮衍生物环组成,但其中一个在 2-硫代海因核心的 N3 原子上富集了一个乙酸基团。这些化合物的抗菌性能通过系列稀释法进行了测试,以获得 MIC。还研究了蓝光照射对测试化合物的影响。通过比较法,以 periaphthenone (PN) 为标准,确定了 420nm 激发时单线态氧 (O*,Δ) 的相对生成率。在将混合物和置于微量滴定板中的细菌的悬浮液进行蓝光照射后,也研究了抗菌性能。初步结果证实,一些混合化合物对参考革兰氏阳性细菌菌株具有抑菌活性,其中一些化合物对革兰氏阴性细菌也具有抑菌活性。蓝光激活增强了测试化合物的抑菌效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e796/8839260/e279ffcb81e9/molecules-27-01069-sch001.jpg

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