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SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.
Chopko TC, Han C, Gregro AR, Engers DW, Felts AS, Poslusney MS, Bollinger KA, Morrison RD, Bubser M, Lamsal A, Luscombe VB, Cho HP, Schnetz-Boutaud NC, Rodriguez AL, Chang S, Daniels JS, Stec DF, Niswender CM, Jones CK, Wood MR, Wood MW, Duggan ME, Brandon NJ, Conn PJ, Bridges TM, Lindsley CW, Melancon BJ. Chopko TC, et al. Among authors: wood mr. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2224-2228. doi: 10.1016/j.bmcl.2019.06.032. Epub 2019 Jun 20. Bioorg Med Chem Lett. 2019. PMID: 31248774 Free PMC article.
VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.
Engers DW, Melancon BJ, Gregro AR, Bertron JL, Bollinger SR, Felts AS, Konkol LC, Wood MR, Bollinger KA, Luscombe VB, Rodriguez AL, Jones CK, Bubser M, Yohn SE, Wood MW, Brandon NJ, Dugan ME, Niswender CM, Conn PJ, Bridges TM, Lindsley CW. Engers DW, et al. Among authors: wood mr. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1714-1718. doi: 10.1016/j.bmcl.2019.05.026. Epub 2019 May 16. Bioorg Med Chem Lett. 2019. PMID: 31113706
Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands.
Poslusney MS, Salovich JM, Wood MR, Melancon BJ, Bollinger KA, Luscombe VB, Rodriguez AL, Engers DW, Bridges TM, Niswender CM, Conn PJ, Lindsley CW. Poslusney MS, et al. Among authors: wood mr. Bioorg Med Chem Lett. 2019 Feb 1;29(3):362-366. doi: 10.1016/j.bmcl.2018.12.039. Epub 2018 Dec 18. Bioorg Med Chem Lett. 2019. PMID: 30580918 Free PMC article.
Corrigendum to "Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184].
Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Jeffrey Conn P, Bridges TM, Lindsley CW. Tarr JC, et al. Among authors: wood mr. Bioorg Med Chem Lett. 2018 Sep 15;28(17):3014. doi: 10.1016/j.bmcl.2018.07.022. Epub 2018 Jul 31. Bioorg Med Chem Lett. 2018. PMID: 30076050 Free PMC article. No abstract available.
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.
Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW. Tarr JC, et al. Among authors: wood mr. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5179-5184. doi: 10.1016/j.bmcl.2017.10.053. Epub 2017 Oct 24. Bioorg Med Chem Lett. 2017. PMID: 29089231 Free PMC article.
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.
Tarr JC, Wood MR, Noetzel MJ, Bertron JL, Weiner RL, Rodriguez AL, Lamsal A, Byers FW, Chang S, Cho HP, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW. Tarr JC, et al. Among authors: wood mr. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2990-2995. doi: 10.1016/j.bmcl.2017.05.014. Epub 2017 May 6. Bioorg Med Chem Lett. 2017. PMID: 28522253 Free PMC article.
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