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Page 1
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: siuciak ja. 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
Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia.
Helal CJ, Kang Z, Hou X, Pandit J, Chappie TA, Humphrey JM, Marr ES, Fennell KF, Chenard LK, Fox C, Schmidt CJ, Williams RD, Chapin DS, Siuciak J, Lebel L, Menniti F, Cianfrogna J, Fonseca KR, Nelson FR, O'Connor R, MacDougall M, McDowell L, Liras S. Helal CJ, et al. J Med Chem. 2011 Jul 14;54(13):4536-47. doi: 10.1021/jm2001508. Epub 2011 Jun 8. J Med Chem. 2011. PMID: 21650160
1-[(1-methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 positive allosteric modulators for the treatment of psychosis.
Zhang L, Brodney MA, Candler J, Doran AC, Duplantier AJ, Efremov IV, Evrard E, Kraus K, Ganong AH, Haas JA, Hanks AN, Jenza K, Lazzaro JT, Maklad N, McCarthy SA, Qian W, Rogers BN, Rottas MD, Schmidt CJ, Siuciak JA, Tingley FD 3rd, Zhang AQ. Zhang L, et al. Among authors: siuciak ja. J Med Chem. 2011 Mar 24;54(6):1724-39. doi: 10.1021/jm101414h. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366332
3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization.
Duplantier AJ, Efremov I, Candler J, Doran AC, Ganong AH, Haas JA, Hanks AN, Kraus KG, Lazzaro JT Jr, Lu J, Maklad N, McCarthy SA, O'Sullivan TJ, Rogers BN, Siuciak JA, Spracklin DK, Zhang L. Duplantier AJ, et al. Among authors: siuciak ja. Bioorg Med Chem Lett. 2009 May 1;19(9):2524-9. doi: 10.1016/j.bmcl.2009.03.032. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19328692
Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia.
Schmidt CJ, Chapin DS, Cianfrogna J, Corman ML, Hajos M, Harms JF, Hoffman WE, Lebel LA, McCarthy SA, Nelson FR, Proulx-LaFrance C, Majchrzak MJ, Ramirez AD, Schmidt K, Seymour PA, Siuciak JA, Tingley FD 3rd, Williams RD, Verhoest PR, Menniti FS. Schmidt CJ, et al. Among authors: siuciak ja. J Pharmacol Exp Ther. 2008 May;325(2):681-90. doi: 10.1124/jpet.107.132910. Epub 2008 Feb 20. J Pharmacol Exp Ther. 2008. PMID: 18287214
48 results