5212
B. K. Albrecht et al. / Bioorg. Med. Chem. Lett. 18 (2008) 5209–5212
5. (a) Jensen, A. A.; Frolund, B.; Liljefors, T.; Krogsgaard-Larsen, P. J. Med.
In summary, a series of potent and selective small molecule
4b2 nAChR potentiators have been reported. These compounds
show excellent CNS-penetration and good activity against the hu-
man and rat 4b2 nAChR clone. A lead series with good CNS proper-
ties has allowed for testing of the potentiator mechanism in animal
models of disease, studies that will be reported in due course.
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337.
ha
a
6. For some recent reports on selective
a4b2 nAChR selective agonists see (a)
Bunnelle, W. H.; Daanen, J. F.; Ryther, K. B.; Schrimpf, M. R.; Dart, M. J.;
Gelain, A.; Meyer, M. D.; Frost, J. M.; Anderson, D. J.; Buckley, M.; Curzon, P.;
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David, J.; Faltynek, C.; Dyhring, T.; Ahring Philip, K.; Rueter Lynne, E.;
Curzon, P.; Buckley Michael, J.; Marsh Kennan, C.; Kempf-Grote, A.; Meyer
Michael, D. Biochem. Pharmacol. 2007, 74, 1253; (d) Ji, J.; Schrimpf, M. R.;
Sippy, K. B.; Bunnelle, W. H.; Li, T.; Anderson, D. J.; Faltynek, C.; Surowy, C.
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Acknowledgments
The authors thank Steve Hollis for NMR assistance and struc-
tural assignments.
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