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Helloana Azevedo-Barbosa Bianca Pereira do Vale Grazielle Guidolin Rossi Fallon dos Santos Siqueira Kevim Bordignon Guterres Marli Matiko Anraku de Campos Thiago dos Santos Jamie Anthony Hawkes Danielle Ferreira Dias Stefânia Neiva Lavorato Thiago Belarmino de Souza Diogo Teixeira Carvalho 《化学与生物多样性》2021,18(5):e2100066
Using molecular hybridization, specific sulfonamide derivatives of eugenol were synthesized with subtle modifications in the allylic chain of the eugenol subunit (and also in the nature of the substituent group in the sulfonamide aromatic ring) which allowed us to study the influence of structural changes on the antimicrobial potential of the hybrids. Antimicrobial test results showed that most of the synthesized hybrid compounds showed good activity with better results than the parent compounds. Molecular docking studies of the hybrids with the essential bacterial enzyme DHPS showed complexes with low binding energies, suggesting that DHPS could be a possible target for the antibacterial sulfonamide-eugenol hybrids. Furthermore, most of the final compounds presented similar docking poses to that of the crystallographic ligand sulfamethoxazole. The results obtained allow us to conclude that these are promising compounds for use as new leads in the search for new antibacterial sulfonamides. 相似文献
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