1.
Bioorg Med Chem Lett
; 29(9): 1085-1089, 2019 05 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-30850166
RESUMO
Targeted covalent inhibitors of urease were developed on the basis of the catechol structure. Forty amide and ester derivatives of 3,4-dihydroxyphenylacetic acid, caffeic acid, ferulic acid and gallic acid were obtained and screened against Sporosarcinia pasteurii urease. The most active compound, namely propargyl ester of 3,4-dihydroxyphenylacetic acid exhibited IC50â¯=â¯518â¯nM andkinact/Kiâ¯=â¯1379â¯M-1â¯s-1. Inhibitory activity of this compound was better and toxicity lower than those obtained for the starting compound - catechol. The molecular modelling studies revealed a mode of binding consistent with structure-activity relationships.