Synthesis and Antimicrobial Activity of Novel 4-Hydroxy-2-quinolone Analogs

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2020 Jul 9

PMID 32635479

Citations 8

Authors

Thitiphong Khamkhenshorngphanuch

Kittipat Kulkraisri

Alongkorn Janjamratsaeng

Napasawan Plabutong

Arsa Thammahong

Kanitta Manadee

Sarisa Na Pombejra

Tanatorn Khotavivattana

Affiliations

Soon will be listed here.

Abstract

Alkyl quinolone has been proven to be a privileged scaffold in the antimicrobial drug discovery pipeline. In this study, a series of new 4-hydroxy-2-quinolinone analogs containing a long alkyl side chain at C-3 and a broad range of substituents on the C-6 and C-7 positions were synthesized. The antibacterial and antifungal activities of these analogs against , , and were investigated. The structure-activity relationship study revealed that the length of the alkyl chain, as well as the type of substituent, has a dramatic impact on the antimicrobial activities. Particularly, the brominated analogs with a nonyl side chain exhibited exceptional antifungal activities against (half maximal inhibitory concentration (IC) = 1.05 µg/mL), which surpassed that of the amphotericin B used as a positive control. The antibacterial activity against , although not as potent, showed a similar trend to the antifungal activity. The data suggest that the 4-hydroxy-2-quinolone is a promising framework for the further development of new antimicrobial agents, especially for antifungal treatment.

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