89999-90-6Relevant articles and documents
Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders
Xu, Heng,Lu, Hongfu,Xu, Zhongmiao,Luan, Linbo,Li, Chengyong,Xu, Yan,Dong, Kelly,Zhang, Jinqiang,Li, Xiong,Li, Yvonne,Liu, Gentao,Gong, Sophie,Zhao, Yong-Gang,Liu, Ailian,Zhang, Yueting,Zhang, Wei,Cai, Xin,Xiang, Jia-Ning,Elliott, John D.,Lin, Xichen
supporting information, p. 397 - 402 (2016/05/19)
Structure-activity relationship exploration of the historical biarylurea series led to the identification of novel CNS penetrant CXCR2 antagonists with nanomolar potency, favorable PK profile, and good developability potentials. More importantly, the key
Synthesis of the calcilytic ligand NPS 2143
Johansson, Henrik,Cailly, Thomas,Thomsen, Alex Rojas Bie,Braeuner-Osborne, Hans,Pedersen, Daniel Sejer
, p. 1383 - 1387 (2013/08/23)
(R)-3 (NPS 2143) is a negative allosteric modulator of the human calcium-sensing receptor (CaSR) and as such represents an important pharmacological tool compound for studying the CaSR. Herein, we disclose for the first time a complete experimental description, detailed characterisation and assessment of enantiomeric purity for (R)-3. An efficient, reproducible and scalable synthesis of (R)-3 that requires a minimum of chromatographic purification steps is presented. (R)-3 was obtained in excellent optical purity (er > 99:1) as demonstrated by chiral HPLC and the pharmacological profile for (R)-3 is in full accordance with that reported in the literature.
Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor β
Minutolo, Filippo,Bellini, Rosalba,Bertini, Simone,Carboni, Isabella,Lapucci, Annalina,Pistolesi, Letizia,Prota, Giovanni,Rapposelli, Simona,Solati, Francesca,Tuccinardi, Tiziano,Martinelli, Adriano,Stossi, Fabio,Carlson, Kathryn E.,Katzenellenbogen, Benita S.,Katzenellenbogen, John A.,Macchia, Marco
, p. 1344 - 1351 (2008/09/21)
Salicylaldoximes possess a hydrogen-bonded pseudocyclic A′ ring in place of the typical phenolic A ring that is characteristic of most estrogen receptor (ER) ligands. Monoaryl-substituted salicylaldoximes were obtained by replacing the phenol moiety (ring
