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Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening
Applied Sciences ( IF 2.5 ) Pub Date : 2021-01-27 , DOI: 10.3390/app11031180
Kinga Paruch , Łukasz Popiołek , Anna Biernasiuk , Anna Berecka-Rycerz , Anna Malm , Anna Gumieniczek , Monika Wujec

Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound 15, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL.

中文翻译:

4-甲基-1,2,3-噻二唑-5-羧酸酰肼的新型衍生物:合成,亲脂性和体外抗菌活性筛选

细菌感染,尤其是那些由对常用抗生素和化学治疗药具有抗性的菌株引起的细菌感染,仍然是当前对公共健康的威胁。因此,寻找具有潜在抗菌活性的新分子是重要的研究目标。在本文中,我们介绍了一系列合成的和评估的一系列15种4-甲基-1,2,3-噻二唑-5-羧酸新衍生物的体外抗菌活性。主要观察到新化合物对革兰氏阳性细菌的潜在抗菌作用。具有5-硝基-2-呋喃基部分的化合物15具有最高的生物活性:最小抑菌浓度(MIC)= 1.95–15.62 µg / mL,最小杀菌浓度(MBC)/ MIC = 1–4 µg / mL。
更新日期:2021-01-27
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