The discovery of 2-fluoro-N-(3-fluoro-4-(5-((4-morpholinobutyl)amino)-1,3, 4-oxadiazol-2-yl)phenyl)benzamide, a full agonist of the alpha-7 nicotinic acetylcholine receptor showing efficacy in the novel object recognition model of cognition enhancement

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 10, 2012, Pages 3531-3534

  Skidmore, John ^a,f   Atcha, Zeenat ^b   Boucherat, Emmanuelle ^a   Castelletti, Laura ^c   Chen, Deborah W ^b   Coppo, Frank T ^d   Cutler, Leanne ^a   Dunsdon, Rachel M ^a   Heath, Bronagh M ^a   Hutchings, Rio ^a   Hurst, David N ^a   Javed, Sahar ^a   Martin, Samuel ^a   Maskell, Emma S L ^e   Norton, David ^a   Pemberton, Darrel J ^b,h   Redshaw, Sally ^a,g   Rutter, Richard ^b   Sehmi, Sanjeet S ^a   Scoccitti, Tiziana ^a   Temple, Hannah E ^a   Theobald, Pam ^a   Ward, Robert W ^a   Wilson, David M ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

^b GLAXOSMITHKLINE   (China)

^c GSK   (Italy)

^d GLAXOSMITHKLINE   (United States)

^e Cell Biology Unit   (United Kingdom)

^f UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^g DDO Limited   (United Kingdom)

^h Neurosciences Division Johnson and Johnson PRF   (Belgium)

Author keywords

7 Nicotinic acetylcholine receptor agonists; Alzheimer's disease; Cognition; Oxadiazole

Indexed keywords

2 FLUORO N [3 FLUORO 4 [5 [(4 MORPHOLINOBUTYL)AMINO] 1,3 4 OXADIAZOL 2 YL]PHENYL]BENZAMIDE; 5 (8 AMINO 7 CHLORO 2,3 DIHYDRO 1,4 BENZODIOXIN 5 YL) 3 [1 (2 PHENYLETHYL) 4 PIPERIDINYL] 1,3,4 OXADIAZOL 2(3H) ONE; ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR AGONIST; BUNGAROTOXIN RECEPTOR; CHOLINERGIC RECEPTOR STIMULATING AGENT; PARTIAL AGONIST; POTASSIUM CHANNEL HERG; SEROTONIN 4 AGONIST; SL 65 0155; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CARDIOVASCULAR RISK; COGNITION; CONTROLLED STUDY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SELECTIVITY; MODEL; MOUSE; NONHUMAN; RAT; RECOGNITION; STRUCTURE ACTIVITY RELATION;

ANIMALS; COGNITION; DOSE-RESPONSE RELATIONSHIP, DRUG; NICOTINIC AGONISTS; RABBITS; RECEPTORS, NICOTINIC;

EID: 84860476417     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.03.062     Document Type: Article

References (14)

1. J. Skidmore Bioorg. Med. Chem. Lett. 2012 http://dx.doi.org/10.1016/j. bmcl.2012.03.040
2. M.J. Curtis J. Pharmacol. Toxicol. 49 2004 217
3. H. Guthrie, F.S. Livingston, U. Gubler, and R. Garippa J. Biomol. Screen. 10 2005 832
4. Q. Wang, J.D. Rager, K. Weinstein, P.S. Kardos, G.L. Dobson, J. Li, and I.J. Hidalgo Int. J. Pharm. 288 2005 349
5. S.G. Summerfield, A.J. Stevens, L. Cutler, M. Osuna, B. Hammond, S.P. Tang, A. Hersey, D.J. Spalding, and P. Jeffrey Pharmacol. Exp. Ther. 316 2006 1282
6. Coppo, F. T.; Maskell, E. S. L.; Redshaw, S.; Skidmore, J.; Ward, R. W.; Wilson, D. M. WO2007138033.
7. C. Jamieson, E.M. Moir, Z. Rankovic, and G. Wishart J. Med. Chem. 49 2006 5029
8. Y. Zhang, and L.Z. Benet Clin. Pharmacokinet. 40 2001 159
9. Z. Atcha, W.S. Chen, A.B. Ong, F.K. Wong, A. Neo, E.R. Browne, J. Witherington, and D.J. Pemberton Psychopharmacol. (Berl.) 200 2009 415
10. D.P. Goh, A.H. Neo, C.W. Goh, C.C. Aw, L.S. New, W.S. Chen, Z. Atcha, E.R. Browne, and E.C. Chan J. Proteome Res. 8 2009 5679
11. P.C. Moser, O.E. Bergis, S. Jegham, A. Lochead, J. Terranova, E. Duconseille, D. Caille, I. Berque-Bestel, F. Lezoualc'h, R. Fischmeister, A. Dumuis, J. Bockaert, P. George, P. Soubrié, and B. Scatton J Pharmacol. Exp. Ther. 302 2002 731
12. L.M. Hondeghem, L. Carlsson, and G. Duker Circulation 103 2001 2004
13. L.M. Hondeghem, and P. Hoffmann J. Cardiovas. Pharm. 41 2003 14
14. C. Virginio, A. Giacometti, A. Aldegheri, J.M. Rimland, and G.C. Terstappen Eur. J. Pharmacol. 445 2002 153