EVALUATION OF ANTIBACTERIAL ACTIVITY 5-AMINO-3-METHYLISOXAZOLE-4-CARBOHYDRAZIDE AND 5-AMINOISOXAZOLE[5,4-d]PYRIMIDIN-4-ONE DERIVATIVES

IF 0.4 4区医学 Q4 PHARMACOLOGY & PHARMACY

Acta poloniae pharmaceutica Pub Date : 2023-05-04 DOI:10.32383/appdr/162790

M. Mączyński, A. Regiec, Paulina Płoszaj, Miroslawa Kacaniova, A. Piwowar

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引用次数: 0

Abstract

Searching for new compounds with specific biological activity in relation to various bacterial strains due to the increasing number of bacterial infections and the frequently developing antimicrobial resistance (AMR) is a significant problem in healthcare. Based on previous promising research related to the activity of isoxazole-4-carbohydrazide derivatives, we currently examined different substituted isoxazole-4-carbohydrazide derivatives in vitro against a panel of bacterial strains. In this work we evaluated antibacterial activity of 30 derivatives, previously described as mildly antimycobacterial, in 10 bacterial strains (5 Gram-negative (G-) and Gram-postive (G+) bacterias). Based on minimum inhibitory concentration (MIC), the mainly MIC50 and MIC90 values, the tested derivatives generally have shown rather weak and mild antibacterial activity. The most active compounds were 3d and 4d, both with methyl substituent in benzene ring. More detailed examination should be continued but this research increased the library of isoxazole derivatives with broad biological activity.

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5-氨基-3-甲基异恶唑-4-羧酸和5-氨基异恶唑[5,4-d]嘧啶-4-酮衍生物的抗菌活性评价

由于细菌感染数量的增加和频繁出现的抗微生物耐药性（AMR），寻找与各种菌株具有特定生物活性的新化合物是医疗保健中的一个重大问题。基于先前与异恶唑-4-碳酰肼衍生物活性相关的有前景的研究，我们目前在体外检测了不同取代的异恶唑4-碳酰肼衍生品对一组细菌菌株的作用。在这项工作中，我们评估了30种衍生物在10种细菌菌株（5种革兰氏阴性（G-）和革兰氏阳性（G+）细菌）中的抗菌活性，这些衍生物以前被描述为轻度抗分枝杆菌。基于最小抑菌浓度（MIC），主要是MIC50和MIC90值，测试的衍生物通常显示出相当弱和温和的抗菌活性。活性最高的化合物是3d和4d，它们都在苯环上有甲基取代基。应该继续进行更详细的检查，但这项研究增加了具有广泛生物活性的异恶唑衍生物的库。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Acta poloniae pharmaceutica 医学-药学

CiteScore

0.80

自引率

0.00%

发文量

审稿时长

6-12 weeks

期刊介绍： The international journal of the Polish Pharmaceutical Society is published in 6 issues a year. The journal offers Open Access publication of original research papers, short communications and reviews written in English, in all areas of pharmaceutical sciences. The following areas of pharmaceutical sciences are covered: Analysis, Biopharmacy, Drug Biochemistry, Drug Synthesis, Natural Drugs, Pharmaceutical Technology, Pharmacology and General. A bimonthly appearing in English since 1994, which continues “Acta Poloniae Pharmaceutica”, whose first issue appeared in December 1937. The war halted the activity of the journal’s creators. Issuance of “Acta Poloniae Pharmaceutica” was resumed in 1947. From 1947 the journal appeared irregularly, initially as a quarterly, then a bimonthly. In the years 1963 – 1973 alongside the Polish version appeared the English edition of the journal. Starting from 1974 only works in English are published in the journal. Since 1995 the journal has been appearing very regularly in two-month intervals (six books a year). The journal publishes original works from all fields of pharmacy, summaries of postdoctoral dissertations and laboratory notes.