Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain

A novel series of N-type calcium channel inhibitors have been discovered. Optimization of potency and HT-ADME properties provides 4-aminocyclopentapyrrolidines with analgesic efficacy after oral dosing.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-09, Vol.23 (17), p.4857-4861
Hauptverfasser:	Beebe, Xenia, Yeung, Clinton M., Darczak, Daria, Shekhar, Shashank, Vortherms, Timothy A., Miller, Loan, Milicic, Ivan, Swensen, Andrew M., Zhu, Chang Z., Banfor, Patricia, Wetter, Jill M., Marsh, Kennan C., Jarvis, Michael F., Scott, Victoria E., Schrimpf, Michael R., Lee, Chih-Hung
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Analgesia Analgesics Analgesics - chemical synthesis Analgesics - chemistry Analgesics - metabolism Analgesics - therapeutic use Animals Calcium Channel Blockers - chemical synthesis Calcium Channel Blockers - chemistry Calcium Channel Blockers - metabolism Calcium Channel Blockers - therapeutic use calcium channels Calcium Channels, N-Type - metabolism chemistry Enantiomeric synthesis Humans Microsomal stability Microsomes - metabolism N-type calcium channels Neuralgia - drug therapy pain Rats SAR Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A novel series of N-type calcium channel inhibitors have been discovered. Optimization of potency and HT-ADME properties provides 4-aminocyclopentapyrrolidines with analgesic efficacy after oral dosing.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2013.06.074