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© 2022 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.

Abstract

Two subseries of aminated quinolinequinones (AQQs, AQQ116) containing electron-withdrawing group (EWG) or electron-donating group (EDG) in aryl amine moiety were successfully synthesized. Antimicrobial activity assessment indicates that some of the AQQs (AQQ810 and AQQ1214) with an EDG in aryl amine exhibited strong antibacterial activity against Gram-positive bacterial strains, including Staphylococcus aureus (ATCC® 29213) and Enterococcus faecalis (ATCC® 29212). In contrast, AQQ4 with an EWG in aryl amine displayed excellent antifungal activity against fungi Candida albicans (ATCC® 10231) with a MIC value of 1.22 μg/mL. To explore the mode of action, the selected AQQs (AQQ4 and AQQ9) were further evaluated in vitro to determine their antimicrobial activity against each of 20 clinically obtained resistant strains of Gram-positive bacteria by performing antibiofilm activity assay and time-kill curve assay. In addition, in silico studies were carried out to determine the possible mechanism of action observed in vitro. The data obtained from these experiments suggests that these molecules could be used to target pathogens in different modes of growth, such as planktonic and biofilm.

Details

Title
Highly Active Small Aminated Quinolinequinones against Drug-Resistant Staphylococcus aureus and Candida albicans
Author
Yıldırım, Hatice 1   VIAFID ORCID Logo  ; Bayrak, Nilüfer 1 ; Yıldız, Mahmut 2 ; Yılmaz, Fatıma Nur 3 ; Mataracı-Kara, Emel 3   VIAFID ORCID Logo  ; Shilkar, Deepak 4   VIAFID ORCID Logo  ; Venkatesan Jayaprakash 4   VIAFID ORCID Logo  ; Amaç Fatih TuYuN 5   VIAFID ORCID Logo 

 Department of Chemistry, Engineering Faculty, Istanbul University-Cerrahpasa, Avcilar, Istanbul 34320, Turkey; [email protected] (H.Y.); [email protected] (N.B.) 
 Department of Chemistry, Gebze Technical University, Gebze, Kocaeli 41400, Turkey; [email protected] 
 Department of Pharmaceutical Microbiology, Pharmacy Faculty, Istanbul University, Beyazit, Istanbul 34116, Turkey; [email protected] (F.N.Y.); [email protected] (E.M.-K.) 
 Department of Pharmaceutical Sciences & Technology, Birla Institute of Technology, Mesra, Ranchi 835 215, Jharkhand, India; [email protected] (D.S.); [email protected] (V.J.) 
 Department of Chemistry, Faculty of Science, Istanbul University, Fatih, Istanbul 34116, Turkey 
First page
2923
Publication year
2022
Publication date
2022
Publisher
MDPI AG
e-ISSN
14203049
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2663049757
Copyright
© 2022 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.