Synthesis of Chiral 3,4-Disubstituted Pyrrolidines with Antibacterial Properties

被引：9

作者：

Rodriguez, Lenka ^{[1
]}

Fisera, Roman ^{[1
]}

Gaalova, Barbora ^{[2
]}

Koci, Kamila ^{[2
]}

Bujdakova, Helena ^{[2
]}

Meciarova, Maria ^{[3
]}

Gorova, Renata ^{[4
]}

Jurdakova, Helena ^{[4
]}

Sebesta, Radovan ^{[3
]}

机构：

[1] SYNKOLA Ltd, Ilkovicova 6, Bratislava 84215, Slovakia

[2] Comenius Univ, Fac Nat Sci, Dept Microbiol, Ilkovicova 6, Bratislava 84215, Slovakia

[3] Comenius Univ, Fac Nat Sci, Dept Organ Chem, Ilkovicova 6, Bratislava 84215, Slovakia

[4] Comenius Univ, Fac Nat Sci, Inst Chem, Ilkovicova 6, Bratislava 84215, Slovakia

来源：

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY | 2020年 / 2020卷 / 17期

关键词：

Asymmetric Organocatalysis; Michael addition; Reductive Cyclization; Pyrrolidine; Antibacterial Activity; ORGANOCATALYTIC MICHAEL ADDITIONS; SILYL ETHERS; ANTIBIOTIC-RESISTANCE; AZOMETHINE YLIDES; ALDEHYDES; DERIVATIVES; CATALYSTS; NITROALKENES; OXYACETALDEHYDES; NITROOLEFINS;

D O I：

10.1002/ejoc.202000235

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Chiral aliphatic heterocycles are important structural feature of many pharmaceutical agents. Antibiotic resistance is a serious medical problem, therefore new antibacterial compounds are urgently needed. Herein, we describe synthesis of a series of 3,4-disubstituted pyrrolidine derivatives via organocatalytic Michael addition followed by reductive cyclization. These compounds inhibited growth of standard as well as methicillin-resistant strains of Escherichia coli and Staphylococcus aureus.

引用

页码：2565 / 2575

页数：11

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