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Page 1
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. Among authors: liras s. J Med Chem. 2011 Jul 14;54(13):4536-47. doi: 10.1021/jm2001508. Epub 2011 Jun 8. J Med Chem. 2011. PMID: 21650160
Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia.
Verhoest PR, Chapin DS, Corman M, Fonseca K, Harms JF, Hou X, Marr ES, Menniti FS, Nelson F, O'Connor R, Pandit J, Proulx-Lafrance C, Schmidt AW, Schmidt CJ, Suiciak JA, Liras S. Verhoest PR, et al. Among authors: liras s. J Med Chem. 2009 Aug 27;52(16):5188-96. doi: 10.1021/jm900521k. J Med Chem. 2009. PMID: 19630403
Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.
Verhoest PR, Proulx-Lafrance C, Corman M, Chenard L, Helal CJ, Hou X, Kleiman R, Liu S, Marr E, Menniti FS, Schmidt CJ, Vanase-Frawley M, Schmidt AW, Williams RD, Nelson FR, Fonseca KR, Liras S. Verhoest PR, et al. Among authors: liras s. J Med Chem. 2009 Dec 24;52(24):7946-9. doi: 10.1021/jm9015334. J Med Chem. 2009. PMID: 19919087
Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.
Verhoest PR, Fonseca KR, Hou X, Proulx-Lafrance C, Corman M, Helal CJ, Claffey MM, Tuttle JB, Coffman KJ, Liu S, Nelson F, Kleiman RJ, Menniti FS, Schmidt CJ, Vanase-Frawley M, Liras S. Verhoest PR, et al. Among authors: liras s. J Med Chem. 2012 Nov 8;55(21):9045-54. doi: 10.1021/jm3007799. Epub 2012 Jul 25. J Med Chem. 2012. PMID: 22780914
Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.
Claffey MM, Helal CJ, Verhoest PR, Kang Z, Fors KS, Jung S, Zhong J, Bundesmann MW, Hou X, Lui S, Kleiman RJ, Vanase-Frawley M, Schmidt AW, Menniti F, Schmidt CJ, Hoffman WE, Hajos M, McDowell L, O'Connor RE, Macdougall-Murphy M, Fonseca KR, Becker SL, Nelson FR, Liras S. Claffey MM, et al. Among authors: liras s. J Med Chem. 2012 Nov 8;55(21):9055-68. doi: 10.1021/jm3009635. Epub 2012 Oct 12. J Med Chem. 2012. PMID: 23025719
Biaryl piperidines as potent and selective delta opioid receptor ligands.
Liras S, McHardy SF, Allen MP, Segelstein BE, Heck SD, Bryce DK, Schmidt AW, Vanase-Frawley M, Callegari E, McLean S. Liras S, et al. Bioorg Med Chem Lett. 2010 Jan 15;20(2):503-7. doi: 10.1016/j.bmcl.2009.11.113. Epub 2009 Nov 26. Bioorg Med Chem Lett. 2010. PMID: 20015649
Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.
Darout E, Robinson RP, McClure KF, Corbett M, Li B, Shavnya A, Andrews MP, Jones CS, Li Q, Minich ML, Mascitti V, Guimarães CR, Munchhof MJ, Bahnck KB, Cai C, Price DA, Liras S, Bonin PD, Cornelius P, Wang R, Bagdasarian V, Sobota CP, Hornby S, Masterson VM, Joseph RM, Kalgutkar AS, Chen Y. Darout E, et al. Among authors: liras s. J Med Chem. 2013 Jan 10;56(1):301-19. doi: 10.1021/jm301626p. Epub 2012 Dec 31. J Med Chem. 2013. PMID: 23234271
Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).
Verhoest PR, Basak AS, Parikh V, Hayward M, Kauffman GW, Paradis V, McHardy SF, McLean S, Grimwood S, Schmidt AW, Vanase-Frawley M, Freeman J, Van Deusen J, Cox L, Wong D, Liras S. Verhoest PR, et al. Among authors: liras s. J Med Chem. 2011 Aug 25;54(16):5868-77. doi: 10.1021/jm2006035. Epub 2011 Jul 22. J Med Chem. 2011. PMID: 21744827
59 results