New Quinoline Derivatives and their Antimicrobial Potential Against <i>Candida Albicans</i> and <i>Staphylococcus Aureus</i>

Abstract Antimicrobial resistance is a pressing global health concern, demanding the development of novel antimicrobial agents. Quinoline derivatives emerge as promising candidates with their diverse chemical structures and recognized bioactive properties. This study aimed to investigate the antimicrobial potency of newly synthesized quinoline derivatives against Candida albicans and five bacterial strains, which are responsible for various infections and have exhibited varying degrees of antibiotic resistance. A series of quinoline derivatives were synthesized through simple structural modifications, such as the inclusion of nitro, amino, and hydrazino groups, or using the molecular hybridization strategy, involving the combination of quinoline and 1,2,3‐triazoles. None of the compounds showed promising activity against the bacterial strains. However, a promising fungistatic effect was observed against C. albicans . In this test, two of the compounds showed lower MIC values than fluconazole (25 μg/mL). In addition, the most promising compounds showed high affinity for the enzyme lanosterol 14 alpha demethylase, due to the low energy values found (−7.6 and −8.2 kcal/mol). Our study offers new avenues for future drug development in the fight against antimicrobial resistance.

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Publication Details

Journal
ChemistrySelect
Published
2024-09-01
DOI
https://doi.org/10.1002/slct.202401828
Citations
5
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
1.25

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article

New Quinoline Derivatives and their Antimicrobial Potential Against Candida Albicans and Staphylococcus Aureus

Elaine Soares Coimbra, Henrique Marcelo Gualberto Pereira, Rodrigo Luiz Fabri, Natasha Silva Mayrink et al.
5 citations
ChemistrySelect
Synthesis and biological activity
1.25
article

New Quinoline Derivatives and their Antimicrobial Potential Against Candida Albicans and Staphylococcus Aureus

Elaine Soares Coimbra, Henrique Marcelo Gualberto Pereira, Rodrigo Luiz Fabri, Natasha Silva Mayrink, Nícolas Glanzmann, Raíssa Soares Meinel, Matheus Torres Branca, Ari Sérgio de Oliveira Lemos, Adilson David da Silva, Isabelle Karine da Costa Nunes
article en
5 citations

Abstract

Abstract Antimicrobial resistance is a pressing global health concern, demanding the development of novel antimicrobial agents. Quinoline derivatives emerge as promising candidates with their diverse chemical structures and recognized bioactive properties. This study aimed to investigate the antimicrobial potency of newly synthesized quinoline derivatives against Candida albicans and five bacterial strains, which are responsible for various infections and have exhibited varying degrees of antibiotic resistance. A series of quinoline derivatives were synthesized through simple structural modifications, such as the inclusion of nitro, amino, and hydrazino groups, or using the molecular hybridization strategy, involving the combination of quinoline and 1,2,3‐triazoles. None of the compounds showed promising activity against the bacterial strains. However, a promising fungistatic effect was observed against C. albicans . In this test, two of the compounds showed lower MIC values than fluconazole (25 μg/mL). In addition, the most promising compounds showed high affinity for the enzyme lanosterol 14 alpha demethylase, due to the low energy values found (−7.6 and −8.2 kcal/mol). Our study offers new avenues for future drug development in the fight against antimicrobial resistance.

ChemistrySelectVol. 9(36)
Universidade Federal de Juiz de Fora (BR), Universidade Federal do Rio de Janeiro (BR)
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Conselho Nacional de Desenvolvimento Científico e Tecnológico, Fundação de Amparo à Pesquisa do Estado de Minas Gerais
Openalex Percentile: Top 23%
Synthesis and biological activity
1.25
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