1.
Bioorg Med Chem Lett
; 23(23): 6239-42, 2013 Dec 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-24157365
RESUMO
Hit-to-lead medicinal chemistry efforts are described starting from a screening hit 1, leading to a new class of aryl sulfonamide-based MR antagonist, exemplified by 17, that possesses favourable MR binding affinity, selectivity profile against closely related NHRs, physicochemical properties and metabolic stability.
Assuntos
Antagonistas de Receptores de Mineralocorticoides/química , Antagonistas de Receptores de Mineralocorticoides/farmacologia , Sulfonamidas/química , Sulfonamidas/farmacologia , Humanos , Antagonistas de Receptores de Mineralocorticoides/síntese química , Modelos Moleculares , Relação Estrutura-Atividade , Sulfonamidas/síntese química
2.
Bioorg Med Chem Lett
; 23(10): 2955-61, 2013 May 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-23566517
RESUMO
A structurally novel set of inhibitors of bacterial type II topoisomerases with potent in vitro and in vivo antibacterial activity was developed. Dual-targeting ability, hERG inhibition, and pharmacokinetic properties were also assessed.