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  • Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists.

Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists.

Bioorganic & medicinal chemistry letters (2013-10-26)
Kentaro Futatsugi, David W Piotrowski, Agustin Casimiro-Garcia, Shaughn Robinson, Matthew Sammons, Paula M Loria, Mary E Banker, Donna N Petersen, Natalia J Schmidt
PMID24157365
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.