Synthesis, in silico Study and Antimicrobial Evaluation of New Selenoglycolicamides

被引：21

作者：

Souza, Helivaldo D. S. ^{[1
]}

de Sousa, Roxana P. E. ^{[1
]}

Lira, Bruno F. ^{[1
]}

Vilela, Raquel F. ^{[1
]}

Borges, Nathalie H. P. B. ^{[2
]}

de Siqueira-Junior, Jose P. ^{[2
]}

Lima, Edeltrudes O. ^{[3
]}

Jardim, Jeane U. G. ^{[3
]}

da Silva, Gracielle A. T. ^{[3
]}

Barbosa-Filho, Jose M. ^{[3
]}

de Athayde-Filho, Petronio F. ^{[1
]}

机构：

[1] Univ Fed Paraiba, Dept Quim, BR-58051900 Joao Pessoa, Paraiba, Brazil

[2] Univ Fed Paraiba, Dept Biol Mol, BR-58051970 Joao Pessoa, Paraiba, Brazil

[3] Univ Fed Paraiba, Dept Ciencias Farmaceut, BR-58051900 Joao Pessoa, Paraiba, Brazil

来源：

JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY | 2019年 / 30卷 / 01期

关键词：

selenoglycolic acid; selenoglycolicamides; antibacterial activity; antifungal activity; MULTIDRUG-RESISTANCE MDR; ESTIMATE SOLUBILITY; ESCHERICHIA-COLI; DRUG DISCOVERY; EFFLUX PUMPS; SELENYLATION; PERMEABILITY; SELENIUM;

D O I：

10.21577/0103-5053.20180148

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Nine new compounds derived from selenoglycolic acid were synthesized, and their structures were fully characterized by elemental analysis, infrared (IR), H-1 and C-13 nuclear magnetic resonance (NMR). The compounds were evaluated in an in silico study and showed strong to moderate antibacterial activity against several strains of Staphylococcus aureus. In particular. three compounds exhibited excellent antibacterial activity, with minimum inhibitory concentrations (MICs) between 16 and 64 mu g mL(-1). Furthermore, two of the nine compounds showed antifungal activity, with MIC of 1024 and 512 mu g mL(-1). In silico studies of the parameters of Lipinski's rule of five indicate that these compounds have potential to be new drug candidates.

引用

页码：188 / 197

页数：10

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