Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition.
| Autor: | Skidmore J; Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK. js930@cam.ac.uk, Atcha Z, Boucherat E, Castelletti L, Chen DW, Coppo FT, Cutler L, Dunsdon RM, Heath BM, Hutchings R, Hurst DN, Javed S, Martin S, Maskell ES, Norton D, Pemberton DJ, Redshaw S, Rutter R, Sehmi SS, Scoccitti T, Temple HE, Theobald P, Ward RW, Wilson DM |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 May 15; Vol. 22 (10), pp. 3560-3. Date of Electronic Publication: 2012 Mar 16. |
| DOI: | 10.1016/j.bmcl.2012.03.040 |
| Abstrakt: | A series of α7 nicotinic acetylcholine receptor full-agonists with a 1,3,4-oxadiazol-2-amine core has been discovered. Systematic exploration of the structure-activity relationships for both α7 potency and selectivity with respect to interaction with the hERG channel are described. Further profiling led to the identification of compound 22, a potent full agonist showing efficacy in the novel object recognition model of cognition enhancement. (Copyright © 2012 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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