William H Bunnelle1
Karin R Tietje1
1William H Bunnelle
1Karin R Tietje
Tautomerism is a phenomenon well know to most chemists but frequently forgotten when chemistry leaves the bench and enters the computational realm. Through the examination of several examples from the crystallographic literature it can be clearly demonstrated that the tautomeric state of a molecules can strongly affect its nature.
A novel 4-aminocyclopentapyrrolidine series of N-type Ca(2+) 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 Ca(2+) channels. N-type Ca(2+) channel blockade was confirmed using electrophysiological… (More)
A series of potent neuronal nicotinic acetylcholine receptor (nAChR) ligands based on a 3,8-diazabicyclo[4.2.0]octane core have been synthesized and evaluated for affinity and agonist efficacy at the human high affinity nicotine recognition site (halpha4beta2) and in a rat model of persistent nociceptive pain (formalin model). Numerous analogs in this… (More)