Novel functionalized β-nitrostyrenes: Promising candidates for new antibacterial drugs

被引：16

作者：

Boguszewska-Czubara, Anna ^{[1
]}

Kula, Karolina ^{[2
]}

Wnorowski, Artur ^{[3
]}

Biernasiuk, Anna ^{[3
]}

Popiolek, Lukasz ^{[3
]}

Miodowski, Dawid ^{[2
]}

Demchuk, Oleg M. ^{[4
,5
]}

Jasinski, Radomir ^{[2
]}

机构：

[1] Med Univ Lublin, Fac Med, 4A Chodzki Str, PL-20093 Lublin, Poland

[2] Cracow Univ Technol, Inst Organ Chem & Technol, 24 Warszawska Str, PL-31155 Krakow, Poland

[3] Med Univ Lublin, Fac Pharm, 4A Chodzki Str, PL-20093 Lublin, Poland

[4] Pharmaceut Res Inst, 8 Rydygiera Str, PL-01793 Warsaw, Poland

[5] Dept Chem UMCS, 2 M Curie Sklodowska Sq, PL-20031 Lublin, Poland

来源：

SAUDI PHARMACEUTICAL JOURNAL | 2019年 / 27卷 / 04期

关键词：

Conjugated nitroalkenes; Antimicrobial activity; Fungicidal activity; Cytotoxicity; B. subtilis ATCC 6633; HepG2; cells; HaCaT cells; DERIVATIVES; MECHANISM;

D O I：

10.1016/j.jsps.2019.02.007

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The process of searching for new antibacterial agents is more and more challenging due to the increasing drug resistance which has become a major concern in the field of infection management. Our study presents a synthesis and characterization by IR, UV, H-1 NMR and C-13 NMR spectra of a homogenous series of 1-EWG functionalized 2-aryl-1-nitroethenes which could prove good candidates for the replacement of traditional antibacterial drugs In vitro screening against a panel of the reference strains of bacteria and fungi and their cytotoxicity towards cultured human HepG2 and HaCaT cells was performed. Antimicrobial results indicated that four of the synthesized compounds exhibited a significant antimicrobial activity against all tested reference bacteria and fungi belonging to yeasts with a specific and strong activity towards B. subtilis ATCC 6633. Two of these compounds had no detectable cytotoxicity towards the cultured human cell lines, making them promising candidates for new antibacterial drugs. (C) 2019 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.

引用

页码：593 / 601

页数：9

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