1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer

被引：37

作者：

Shetnev, Anton ^{[1
]}

Baykov, Sergey ^{[2
]}

Kalinin, Stanislav ^{[2
]}

Belova, Alexandra ^{[1
]}

Sharoyko, Vladimir ^{[2
]}

Rozhkov, Anton ^{[2
]}

Zelenkov, Lev ^{[2
]}

Tarasenko, Marina ^{[3
]}

Sadykov, Evgeny ^{[4
]}

Korsakov, Mikhail ^{[1
]}

Krasavin, Mikhail ^{[2
]}

机构：

[1] Ushinsky Yaroslavl State Pedag Univ, Pharmaceut Technol Transfer Ctr, 108 Respublikanskaya St, Yaroslavl 150000, Russia

[2] St Petersburg State Univ, Inst Chem, 26 Univ Skii Pr, St Petersburg 198504, Russia

[3] Yaroslavl State Tech Univ, 88 Moscowsky Pr, Yaroslavl 150023, Russia

[4] Russian Acad Sci, Siberian Branch, AE Favorsky Irkutsk Inst Chem, 1 Favorsky Str, Irkutsk 664033, Russia

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2019年 / 20卷 / 07期

基金：

俄罗斯基础研究基金会;

关键词：

1,2, 4-oxadiazole; 2-imidazolines; antibacterial; cytotoxicity; MAO inhibition; OXADIAZOLE CLASS; IN-VITRO; INHIBITORS; IDENTIFICATION; FURAZOLIDONE; EXPLORATION; PERIPHERY; DISCOVERY; DESIGN; VIVO;

D O I：

10.3390/ijms20071699

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Replacement of amide moiety with the 1,2,4-oxadiazole core in the scaffold of recently reported efflux pump inhibitors afforded a novel series of oxadiazole/2-imidazoline hybrids. The latter compounds exhibited promising antibacterial activity on both Gram-positive (Staphylococcus aureus, Bacillus subtilis) and Gram-negative (Escherichia coli, Pseudomonas fluorescens) strains. Furthermore, selected compounds markedly inhibited the growth of certain drug-resistant bacteria. Additionally, the study revealed the antiproliferative activity of several antibacterial frontrunners against pancreas ductal adenocarcinoma (PANC-1) cell line, as well as their type-selective monoamine oxidase (MAO) inhibitory profile.

引用

页数：10

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