1.
Bioorg Med Chem Lett
; 23(23): 6239-42, 2013 Dec 01.
Article
in English
| MEDLINE
| ID: mdl-24157365
ABSTRACT
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.
Subject(s)
Mineralocorticoid Receptor Antagonists/chemistry , Mineralocorticoid Receptor Antagonists/pharmacology , Sulfonamides/chemistry , Sulfonamides/pharmacology , Humans , Mineralocorticoid Receptor Antagonists/chemical synthesis , Models, Molecular , Structure-Activity Relationship , Sulfonamides/chemical synthesis
2.
Bioorg Med Chem Lett
; 23(10): 2955-61, 2013 May 15.
Article
in English
| MEDLINE
| ID: mdl-23566517
ABSTRACT
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.
