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Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.
Cook J, Zusi FC, McDonald IM, King D, Hill MD, Iwuagwu C, Mate RA, Fang H, Zhao R, Wang B, Cutrone J, Ma B, Gao Q, Knox RJ, Matchett M, Gallagher L, Ferrante M, Post-Munson D, Molski T, Easton A, Miller R, Jones K, Digavalli S, Healy F, Lentz K, Benitex Y, Clarke W, Natale J, Siuciak JA, Lodge N, Zaczek R, Denton R, Morgan D, Bristow LJ, Macor JE, Olson RE. Cook J, et al. Among authors: macor je. J Med Chem. 2016 Dec 22;59(24):11171-11181. doi: 10.1021/acs.jmedchem.6b01506. Epub 2016 Dec 13. J Med Chem. 2016. PMID: 27958732
Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin.
Macor JE, Blake J, Fox CB, Johnson C, Koe BK, Lebel LA, Morrone JM, Ryan K, Schmidt AW, Schulz DW, et al. Macor JE, et al. J Med Chem. 1992 Nov 13;35(23):4503-5. doi: 10.1021/jm00101a032. J Med Chem. 1992. PMID: 1447752 No abstract available.
(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
Mullen G, Napier J, Balestra M, DeCory T, Hale G, Macor J, Mack R, Loch J 3rd, Wu E, Kover A, Verhoest P, Sampognaro A, Phillips E, Zhu Y, Murray R, Griffith R, Blosser J, Gurley D, Machulskis A, Zongrone J, Rosen A, Gordon J. Mullen G, et al. J Med Chem. 2000 Nov 2;43(22):4045-50. doi: 10.1021/jm000249r. J Med Chem. 2000. PMID: 11063601
154 results