Antimicrobial Activity Derivatives 2H-pirano[2,3-c]piridines against Pathogens of Intestinal Yersiniosis

Q3 Pharmacology, Toxicology and Pharmaceutics Journal of Pharmacy and Nutrition Sciences Pub Date : 2021-10-21 DOI:10.29169/1927-5951.2021.11.11
V. Ivannik, I. Torianyk, T. Moiseienko, A. Skliar, R. Yeromenko, V. Hnatiuk, L. Podrigalo, R. Nazaryan, N.M. Mikhailenko, V. V. Gargin
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Abstract

Background: An important aspect in the treatment of patients with intestinal yersiniosis is the administration of effective antibiotic therapy. Performed research aimed to determine the spectrum and level of antimicrobial activity of 2H-pyrano[2,3- c]pyridine derivatives on the museum and clinical strains of gram-negative microorganisms Yersinia enterocolitica. Methodology: The object of the study was 28 synthetic derivatives of 2H-pyrano[2,3- c]pyridine. The compounds were studied according to their chemical structure. We used the method of serial dilutions in Muller-Hinton liquid nutrient medium with a museum’s and clinical strains of Y.enterocolitica. Results: Studies indicate the promise of further study of the properties of 2H- pyrono[2,3-c]pyridine to create an effective antimicrobial medicine. According to the results of studies on action of antimicrobial compounds synthesized on the basis of 2H-pyrano[2,3-с]pyridine derivatives, it was found that the MIC of compounds for all Y. enterocolitica strains was 100.0 μg/ml. The MBCC of most cultures of Yersinia (72.3 %) was 200.0 μg/ml. Compound 2{3} had a pronounced antiyersiniotic activity, the inhibitory effect of which was manifested at a concentration of 25.0 μg/ml. Retarding the growth of most Yersinia strains (95.3%) with a MIC of 50.0 μg/ml, the MIC of compounds ranged from 50.0 to 200.0 μg/ml. After statistical data processing, pyridine derivatives (compounds 2{3} and 3{5}) were identified, possessing an effective bacteriostatic and bactericidal effect on Y. enterocolitica strains. Conclusions: The results of the research showed a high antimicrobial activity of 2H- pyrano[2,3-c]pyridine derivatives. The highest activity against Y. enterocolitica was found for 2-N2-arylimino-5-hydroxy-methyl-8-methyl-2H-pyrano[2,3-c]pyridine-3-N1- aricarboxamide derivatives.
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2h -吡喃[2,3-c]吡啶衍生物对肠道耶尔森菌病病原菌的抗菌活性研究
背景:治疗肠耶尔森菌病的一个重要方面是给予有效的抗生素治疗。研究2h -吡喃[2,3- c]吡啶衍生物对革兰氏阴性小肠结肠炎耶尔森菌博物馆和临床菌株的抑菌活性谱和水平。方法:以合成的28个2h -吡喃[2,3- c]吡啶衍生物为研究对象。根据化合物的化学结构对它们进行了研究。本研究采用Muller-Hinton液体营养培养基连续稀释的方法,对小肠结肠炎杆菌的博物馆和临床菌株进行了研究。结果表明,进一步研究2H- pyrono[2,3-c]吡啶的性质有望开发出有效的抗菌药物。根据以2h -吡喃[2,3-啶]吡啶衍生物为基础合成的抗菌化合物的作用研究结果,发现化合物对所有小肠结肠炎耶氏菌的MIC均为100.0 μg/ml。大多数培养菌(72.3%)的MBCC为200.0 μg/ml。化合物2{3}具有明显的抑菌活性,浓度为25.0 μg/ml时表现出抑制作用。抑制大部分耶尔森菌生长(95.3%),MIC为50.0 μg/ml,化合物MIC为50.0 ~ 200.0 μg/ml。经统计数据处理,鉴定出吡啶衍生物(化合物2{3}和3{5}),对小肠结肠炎Y.菌株具有有效的抑菌和杀菌作用。结论:研究结果表明,2H-吡喃[2,3-c]吡啶衍生物具有较高的抗菌活性。2- n2 -arylimino-5-羟基-甲基-8-甲基- 2h -pyrano[2,3-c]吡啶-3- n1 - arcarboxamide衍生物对小肠结肠炎的抑制活性最高。
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Journal of Pharmacy and Nutrition Sciences
Journal of Pharmacy and Nutrition Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
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