New aminopropandiol derivatives as orally available and short-acting calcium-sensing receptor antagonists.
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.
Shinagawa
Yuko
Y
Central Pharmaceutical Research Institute, Japan Tobacco Inc., Takatsuki, Osaka, Japan. yuko.shinagawa@jt.com
Inoue
Teruhiko
T
Hirata
Kazuyuki
K
Katsushima
Takeo
T
Nakagawa
Takashi
T
Matsuo
Yushi
Y
Shindo
Masanori
M
Hashimoto
Hiromasa
H
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
D010281:Parathyroid Hormone; D011412:Propanolamines; D044169:Receptors, Calcium-Sensing