3H-Quinazolin-4-ones as a new calcilytic template for the potential treatment of osteoporosis.
Structure-activity relationship studies, focused on identification of the active pharmacophore fragments in a single high-throughput screening calcilytic hit, resulted in the discovery of potent calcium receptor antagonists, substituted 3H-quinazolin-4-ones.
Shcherbakova
Irina
I
Drug Discovery, NPS Pharmaceuticals, Inc., 383 Colorow Drive, Salt Lake City, UT 84108, USA. ishcherbakova@npsp.com
Balandrin
Manuel F
MF
Fox
John
J
Ghatak
Anjan
A
Heaton
William L
WL
Conklin
Rebecca L
RL
D000818:Animals; D008297:Male; D008956:Models, Chemical; D015394:Molecular Structure; D010024:Osteoporosis / Q000188:drug therapy; D010281:Parathyroid Hormone / Q000097:blood; D011799:Quinazolines / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D044169:Receptors, Calcium-Sensing / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
C501908:NPS53574; D010281:Parathyroid Hormone; D011799:Quinazolines; D044169:Receptors, Calcium-Sensing