Microwave-Assisted Synthesis of Diverse Pyrrolo[3,4-c]quinoline-1,3-diones and Their Antibacterial Activities

Title
Microwave-Assisted Synthesis of Diverse Pyrrolo[3,4-c]quinoline-1,3-diones and Their Antibacterial Activities
Author(s)
이용록하립개아크베르이드하야둘라김성홍[김성홍]위영중
Keywords
PROTEIN-KINASE-C; ACRIDONE ALKALOIDS; QUINOLINE DERIVATIVES; ORGANIC-CHEMISTRY; 3-BROMO-4-(1H-3-INDOLYL)-2,5-DIHYDRO-1H-2,5-PYRROLEDIONE DERIVATIVES; ANTIMICROBIAL ACTIVITIES; CASPASE-3 INHIBITORS; ANTI-HIV-1 AGENTS; DRUG DISCOVERY; SOLAR-CELLS
Issue Date
201407
Publisher
AMER CHEMICAL SOC
Citation
ACS COMBINATORIAL SCIENCE, v.16, no.7, pp.333 - 341
Abstract
With the aim of developing a general and practical method for library production, a novel and efficient two-phase microwave-assisted cascade reaction between isatins and beta-ketoamides in [Bmim]BF4/toluene was developed for the synthesis of pyrrolo[3,4-c]quinoline-1,3-diones. The features of this methodology are, the use of microwave-assisted rapid synthesis, mild reaction conditions, high yields, operational simplicity, facile product separation, and recyclability. Furthermore, the antibacterial activities of the pyrrolo[3,4-c]quinoline-1,3-dione derivatives produced were evaluated against Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Enterobacter aerogenes) and Gram-positive bacteria (Bacillus cereus and Staphylococcus aureus). These derivatives showed antibacterial activities against Gram-positive strains that were at least equivalent to that against Gram-negative strains. Compound 7{3,5} displayed the most potent antibacterial activity against P. aeruginosa (MIC = 0.5 mu g/mL) and greater activity than standard ampicillin (MIC = 1 mu g/mL). Compound 7{4,7} exhibited the best inhibitory activity against E. coli and E. aerogenes (MIC = 1 and 0.5 mu g/mL), compared with the standard ampicillin (both MICs = 1 mu g/mL). The synthesized pyrrolo[3,4-c]quinoline-1,3-diones are expected to be widely used as lead compounds for the development of new antibacterial agents.
URI
http://hdl.handle.net/YU.REPOSITORY/31478http://dx.doi.org/10.1021/co500002s
ISSN
2156-8952
Appears in Collections:
공과대학 > 화학공학부 > Articles
자연자원대학 > 식품공학과 > Articles
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE