186201-60-5Relevant articles and documents
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres
Sheffler, Douglas J.,Nedelovych, Michael T.,Williams, Richard,Turner, Stephen C.,Duerk, Brittany B.,Robbins, Megan R.,Jadhav, Sataya B.,Niswender, Colleen M.,Jones, Carrie K.,Conn, P. Jeffrey,Daniels, R. Nathan,Lindsley, Craig W.
, p. 1062 - 1066 (2014/03/21)
This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach, in lieu of an HTS campaign, which provided intellectual property position. Members within this new [3.3.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, and modest CNS penetration. Moreover, enantioselective GlyT1 inhibition was observed, within this novel series and a number of other piperidine bioisosteric cores.
Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca 2+ channel blockers with analgesic activity
Beebe, Xenia,Darczak, Daria,Henry, Rodger F.,Vortherms, Timothy,Janis, Richard,Namovic, Marian,Donnelly-Roberts, Diana,Kage, Karen L.,Surowy, Carol,Milicic, Ivan,Niforatos, Wende,Swensen, Andrew,Marsh, Kennan C.,Wetter, Jill M.,Franklin, Pamela,Baker, Scott,Zhong, Chengmin,Simler, Gricelda,Gomez, Erica,Boyce-Rustay, Janel M.,Zhu, Chang Z.,Stewart, Andrew O.,Jarvis, Michael F.,Scott, Victoria E.
, p. 4128 - 4139 (2012/09/22)
A novel 4-aminocyclopentapyrrolidine series of N-type Ca2+ channel blockers have been discovered. Enantioselective synthesis of the 4-aminocyclopentapyrrolidines was enabled using N-tert-butyl sulfinamide chemistry. SAR studies demonstrate selectivity over L-type Ca2+ channels. N-type Ca2+ channel blockade was confirmed using electrophysiological recording techniques. Compound 25 is an N-type Ca 2+ channel blocker that produces antinociception in inflammatory and nociceptive pain models without exhibiting cardiovascular or motor liabilities.
ANTIBACTERIAL AGENTS
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Page/Page column 19; 28, (2010/10/19)
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment bacterial infections in mammals, particularly humans, are disclosed herein.