600726-61-2Relevant articles and documents
Discovery and structure-activity relationships of trisubstituted pyrimidines/pyridines as novel calcium-sensing receptor antagonists
Yang, Wu,Ruan, Zheming,Wang, Yufeng,Van Kirk, Katy,Zhengping, Ma.,Arey, Brian J.,Cooper, Christopher B.,Seethala, Ramakrishna,Feyen, Jean H. M.,Dickson Jr., John K.
supporting information; experimental part, p. 1204 - 1208 (2009/12/25)
The trisubstituted pyrimidine 1 was identified through high-throughput screening as a novel calcium-sensing receptor (CaSR) antagonist. Small molecule CaSR antagonists and/or negative allosteric modulators have the potential to act as an anabolic agent for the treatment of osteoporosis. The investigation of structure-activity relationships around 1 resulted in the identification of 18c and 18d, which showed efficacy at promoting PTH release in vivo and exhibited improved potency and solubility over the original lead 1.