Premium
Synthesis of Chiral 3,4‐Disubstituted Pyrrolidines with Antibacterial Properties
Author(s) -
Rodriguez Lenka,
Fišera Roman,
Gaálová Barbora,
Koči Kamila,
Bujdáková Helena,
Mečiarová Mária,
Górová Renáta,
Jurdáková Helena,
Šebesta Radovan
Publication year - 2020
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.202000235
Subject(s) - chemistry , pyrrolidine , combinatorial chemistry , escherichia coli , staphylococcus aureus , antibacterial activity , organocatalysis , antibiotics , enantioselective synthesis , organic chemistry , stereochemistry , bacteria , catalysis , biochemistry , genetics , biology , gene
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 .