Exploring the Relationships Between Structure and Antimicrobial Potency of Quinolinequinones

Overview

Journal Antibiotics (Basel)

Specialty Pharmacology

Date 2022 Oct 27

PMID 36290056

Authors

Emel Mataraci-Kara

Nilufer Bayrak

Mahmut Yildiz

Hatice Yildirim

Amac Fatih Tuyun

Affiliations

Soon will be listed here.

Abstract

Microorganisms are responsible for hospital infections, and methicillin-resistant is one of them. In looking for the most effective lead structures to cope with the rise of antimicrobial (antibiotic) resistance, we evaluated the antimicrobial profile of quinolinequinones for potential antimicrobial applications. 1,4-quinone molecules fused with heteroatom have been studied extensively for many years as a source of drugs and lead structures. The aims of this study were to evaluate the antimicrobial activity of quinolinequinones against bacterial and fungal strains, and to probe for potential lead structures. For this reason, the activity of these compounds against three different strains of fungi (, , and ) and Gram-positive and Gram-negative pathogenic bacteria were investigated, searching for potential lead compounds. Five of nine quinolinequinones showed activity mainly against the Gram-positive strains with a minimal inhibitory concentration within the Clinical and Laboratory Standards Institute (CLSI) levels. The results revealed that quinolinequinones have significant activity against bacteria including and , and fungi including and . , , , , and exhibited the highest growth inhibition against two essential species of the Gram-positive strains ( and ). Among these, four molecules (, , , and ) were also active against , the other member of the Gram-positive strains. The antifungal profile of two quinolinequinones ( and ) indicated that they were as effective as the reference drug Clotrimazole against . The same molecules also have potential inhibitory antifungal activity against . For better understanding, the most active two quinolinequinones ( and ) were examined for biofilm inhibition and a time-kill kinetic study.

Citing Articles

Prospects for Prostate Cancer Chemotherapy: Cytotoxic Evaluation and Mechanistic Insights of Quinolinequinones with ADME/PK Profile.

Jannuzzi A, Yilmaz Goler A, Biswas A, Mondal S, Basavanakatti V, Yildirim H Biomedicines. 2024; 12(6).

PMID: 38927448 PMC: 11200585. DOI: 10.3390/biomedicines12061241.

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