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Novel esters derived from 4-hydroxychalcones as potential sunscreens with antimicrobial action.

Authors :
de Sousa, Abraão Pinheiro
Souza, Helivaldo Diógenes da Silva
Almeida-Júnior, Alexandre
da Silva, Marcelo Felipe Rodrigues
Cordeiro, Laísa Vilar
Lima, Edeltrudes de Oliveira
Fiss, Gabriela Fehn
de Athayde-Filho, Petrônio Filgueiras
Source :
Synthetic Communications. 2024, Vol. 54 Issue 12, p973-991. 19p.
Publication Year :
2024

Abstract

Ten novel 4-esterchalcones, licochalcone analogues, were strategically synthesized to study the effect of electro-donating or electro-withdrawing substituents in the aryl enone moiety on their pharmacological and photoprotective properties. 4-Esterchalcones had their drug-like character evaluated, which demonstrated positive characteristics for the development of novel drug candidates. In the in vitro antimicrobial evaluation, isovaleryl 4-esterchalcones showed activity against strains of Staphylococcus aureus, Candida albicans and C. tropicalis with minimum inhibitory concentration (MIC) in the range of 2.64-3.32 µmol mL−1, and the isobutyryl 4-esterchalcone 5d (4'-Br) presented antimicrobial activity against all strains tested, with a MIC of 2.74 µmol mL−1. In the UV-Vis study, λmax were observed at 312-327 nm, the UVB range, mainly. The best SPF-UVB results ranged from 18.04 to 21.06, with high εmax values, indicating that 4-esterchalcones have the potential to act as sunscreens. Furthermore, along with the environmental concern, halogenated compounds demonstrated slightly toxic on Artemia salina. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
00397911
Volume :
54
Issue :
12
Database :
Academic Search Index
Journal :
Synthetic Communications
Publication Type :
Academic Journal
Accession number :
177800171
Full Text :
https://doi.org/10.1080/00397911.2024.2356641