title: New aminopropandiol derivatives as orally available and short-acting calcium-sensing receptor antagonists.
abstract: Synthesis and structure-activity relationship studies on a new aminopropandiol class of derivatives as calcium-sensing receptor antagonists are described. Modification of the phenolic moiety of a calcilytic compound NPS 2143 led to the identification of an orally available compound (R,R)-31 which demonstrated a rapid and transient stimulation of PTH release in rats.
authors.affiliation: Central Pharmaceutical Research Institute, Japan Tobacco Inc., Takatsuki, Osaka, Japan. yuko.shinagawa@jt.com
authors.forename: Yuko
authors.initials: Y
authors.lastname: Shinagawa
authors.forename: Teruhiko
authors.initials: T
authors.lastname: Inoue
authors.forename: Kazuyuki
authors.initials: K
authors.lastname: Hirata
authors.forename: Takeo
authors.initials: T
authors.lastname: Katsushima
authors.forename: Takashi
authors.initials: T
authors.lastname: Nakagawa
authors.forename: Yushi
authors.initials: Y
authors.lastname: Matsuo
authors.forename: Masanori
authors.initials: M
authors.lastname: Shindo
authors.forename: Hiromasa
authors.initials: H
authors.lastname: Hashimoto
mesh_terms: D000818:Animals; D001682:Biological Availability; D010024:Osteoporosis / Q000188:drug therapy; D010281:Parathyroid Hormone / Q000378:metabolism; D011412:Propanolamines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D044169:Receptors, Calcium-Sensing / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
chemical_list: D010281:Parathyroid Hormone; D011412:Propanolamines; D044169:Receptors, Calcium-Sensing