title: Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists.
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.
authors.affiliation: Pfizer Worldwide Research and Development, 620 Memorial Drive, Cambridge, MA 02139, United States. Electronic address: Kentaro.Futatsugi@pfizer.com.
authors.forename: Kentaro
authors.initials: K
authors.lastname: Futatsugi
authors.forename: David W
authors.initials: DW
authors.lastname: Piotrowski
authors.forename: Agustin
authors.initials: A
authors.lastname: Casimiro-Garcia
authors.forename: Shaughn
authors.initials: S
authors.lastname: Robinson
authors.forename: Matthew
authors.initials: M
authors.lastname: Sammons
authors.forename: Paula M
authors.initials: PM
authors.lastname: Loria
authors.forename: Mary E
authors.initials: ME
authors.lastname: Banker
authors.forename: Donna N
authors.initials: DN
authors.lastname: Petersen
authors.forename: Natalia J
authors.initials: NJ
authors.lastname: Schmidt
mesh_terms: D006801:Humans; D000451:Mineralocorticoid Receptor Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000451:Mineralocorticoid Receptor Antagonists; D013449:Sulfonamides
keywords: Aryl sulfonamide; Mineralocorticoid receptor; Nonsteroidal MR antagonist