1.
Synthesis, SAR and molecular docking study of novel non-ß-lactam inhibitors of TEM type ß-lactamase.
Bioorg Med Chem Lett
; 27(7): 1588-1592, 2017 04 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-28237762
RESUMO
The novel classes of acylated phenoxyanilide and thiourea compounds were investigated for their ability to inhibit TEM type ß-lactamase enzyme. Two compounds 4g and 5c reveal the inhibition potency in micromolar range and show their action by non-covalent binding in the vicinity of the TEM-171 active site. The structure activity relationship around carbon chain length and different substituents in ortho- and para-positions of acylated phenoxyanilide as well as molecular modelling study has been performed.