e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino) methyl] piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective …
…, JW Butcher, CF Claiborne, DA Claremon…
Index: Liverton, Nigel J.; Bednar, Rodney A.; Bednar, Bohumil; Butcher, John W.; Claiborne, Christopher F.; Claremon, David A.; Cunninghan, Michael; DiLella, Anthony G.; Gaul, Stanley L.; Libby, Brian E.; Lyie, Elizabeth A.; Lynch, Joseph J.; McCauley, John A.; Mosser, Scott D.; Nguyen, Kevin T.; Stump, Gary L.; Sun, Hong; Wang, Hao; Yergey, James; Koblan, Kenneth S. Journal of Medicinal Chemistry, 2007 , vol. 50, # 4 p. 807 - 819
The discovery of a novel series of NR2B subtype selective N-methyl-d-aspartate (NMDA) antagonists is reported. Initial optimization of a high-throughput screening lead afforded an aminopyridine derivative 13 with significant NR2B antagonist potency but limited selectivity over hERG-channel and other off-target activities. Further structure-activity studies on the aminoheterocycle moiety and optimization of the carbamate led to the highly potent 2- ...
