Design, synthesis, and evaluation of novel 2-substituted 1,4-benzenediol library as antimicrobial agents against clinically relevant pathogens

Lana, Daiane Flores Dalla; Batista, Bruna Gerardon; Machado, Gabriella da Rosa Monte; Teixeira, Mário Lettieri; Oliveira, Luís Flávio Souza de; Machado, Michel Mansur; Andrade, Saulo Fernandes de; Lopes, William; Vainstein, Marilene Henning; Lima, Alejandro Peixoto de Abreu; Pandolfi, Enrique; Silva, Edilma Elayne; Silveira, Gustavo Pozza

doi:10.1016/j.jsps.2019.09.003

Cited by 4 publications

(2 citation statements)

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“…Amongst the 23 compounds designed and synthesized, 17 derivatives have been investigated for inhibitory activity against Gram‐positive strains S. aureus (ATCC 25923, ATCC 33591) and Enterococcus faecalis (ATCC 51299, ATCC 29212) and Gram‐negative bacterial strain E. coli . [ 15 ] In this activity, unfortunately, benzenediol derivatives possessing quinoline motifs have failed to exhibit excellent antibacterial properties. Furthermore, 4‐fluorophenyl analog 10 (Figure 4) out of the sixteen 3‐methylbenzo[ d ]thiazolmethylquinolinium derivatives elicited noteworthy antibacterial properties against drug‐resistant bacterial strains Bacillus subtilis 168, S. aureus ATCC 29213, Enterococcus faecium ATCC 49624, E. faecalis ATCC 29212, Staphylococcus epidermidis ATCC 12228, and E. coli .…”

Section: Antibacterial Activitymentioning

confidence: 99%

“…A weak antifungal activity is noticed for the 6‐chloroquinoline or 6‐fluoroquinoline derivatives appended with dihydroxyphenyl ring at 3‐position. [ 15 ] Decent antifungal potencies are exhibited by the 5‐amino‐7‐bromoquinolin‐8‐yl sulfonate derivatives. [ 23 ] Observation of the zone of inhibition of evaluated quinoline sulfonates has revealed a remarkable inhibitory activity (13 mm) of compound 108 (Figure 16) against fungal strain Aspergillus niger and a slightly diminished activity as compared with fluconazole (15 mm).…”

Section: Antifungal Activitymentioning

confidence: 99%

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Recent update on antibacterial and antifungal activity of quinoline scaffolds

Dorababu¹

2020

Archiv der Pharmazie

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Although most of the heterocycles have been reported to possess a significant pharmacological activity, only a few of them, namely quinoline derivatives, have exhibited the finest biological activities. Despite the few medicinal properties of the plain quinoline molecule, its derivatives exhibit diverse pharmacological properties such as anticancer, anti‐inflammatory, antibacterial, antiviral, antifungal, antiprotozoal activities, and so on. The potential antimicrobial properties of the quinoline derivatives are evident from the decades of research on these derivatives. Owing to limitations like drug resistance, high cost, severe side effects, and less bioavailability of previously synthesized antimicrobial agents, these drugs have become obsolete in recent years. Hence, the design of more efficient antimicrobial drugs must be given topmost priority. A breakthrough in drug discovery is a must to prevent malevolent microbial diseases. Addressing all these issues, researchers have been continuously contributing to antimicrobial drug discovery. Herein, a short description of the pharmacology of antimicrobial agents such as antibacterials and antifungals synthesized recently is provided. The versatile derivatization of the quinoline moiety leading to significant antimicrobial potencies is discussed, considering the structure–activity relationship.

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Section: Antibacterial Activitymentioning

confidence: 99%

Section: Antifungal Activitymentioning

confidence: 99%