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103 results

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Page 1
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: noetzel mj. 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.
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.
Melancon BJ, Lamers AP, Bridges TM, Sulikowski GA, Utley TJ, Sheffler DJ, Noetzel MJ, Morrison RD, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Wood MR. Melancon BJ, et al. Among authors: noetzel mj. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1044-8. doi: 10.1016/j.bmcl.2011.11.110. Epub 2011 Dec 6. Bioorg Med Chem Lett. 2012. PMID: 22197142 Free PMC article.
Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).
Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, Meiler J, Conn PJ, Lindsley CW, Stauffer SR. Turlington M, et al. Among authors: noetzel mj. J Med Chem. 2013 Oct 24;56(20):7976-96. doi: 10.1021/jm401028t. Epub 2013 Oct 9. J Med Chem. 2013. PMID: 24050755 Free PMC article.
Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).
Turlington M, Malosh C, Jacobs J, Manka JT, Noetzel MJ, Vinson PN, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martín-Martín ML, Tong HM, López S, MacDonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Turlington M, et al. Among authors: noetzel mj. J Med Chem. 2014 Jul 10;57(13):5620-37. doi: 10.1021/jm500259z. Epub 2014 Jun 25. J Med Chem. 2014. PMID: 24914612 Free PMC article.
Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.
Turlington M, Noetzel MJ, Bridges TM, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Tong HM, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR. Turlington M, et al. Among authors: noetzel mj. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3641-6. doi: 10.1016/j.bmcl.2014.04.087. Epub 2014 May 2. Bioorg Med Chem Lett. 2014. PMID: 24961642 Free PMC article.
Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.
Bubser M, Bridges TM, Dencker D, Gould RW, Grannan M, Noetzel MJ, Lamsal A, Niswender CM, Daniels JS, Poslusney MS, Melancon BJ, Tarr JC, Byers FW, Wess J, Duggan ME, Dunlop J, Wood MW, Brandon NJ, Wood MR, Lindsley CW, Conn PJ, Jones CK. Bubser M, et al. Among authors: noetzel mj. ACS Chem Neurosci. 2014 Oct 15;5(10):920-42. doi: 10.1021/cn500128b. Epub 2014 Aug 19. ACS Chem Neurosci. 2014. PMID: 25137629 Free PMC article.
Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).
Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Gentry PR, et al. Among authors: noetzel mj. J Med Chem. 2014 Sep 25;57(18):7804-10. doi: 10.1021/jm500995y. Epub 2014 Sep 3. J Med Chem. 2014. PMID: 25147929 Free PMC article.
Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.
Han C, Chatterjee A, Noetzel MJ, Panarese JD, Smith E, Chase P, Hodder P, Niswender C, Conn PJ, Lindsley CW, Stauffer SR. Han C, et al. Among authors: noetzel mj. Bioorg Med Chem Lett. 2015 Jan 15;25(2):384-8. doi: 10.1016/j.bmcl.2014.11.011. Epub 2014 Nov 18. Bioorg Med Chem Lett. 2015. PMID: 25435150 Free PMC article.
Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).
Martín-Martín ML, Bartolomé-Nebreda JM, Conde-Ceide S, Alonso de Diego SA, López S, Martínez-Viturro CM, Tong HM, Lavreysen H, Macdonald GJ, Steckler T, Mackie C, Bridges TM, Daniels JS, Niswender CM, Noetzel MJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Martín-Martín ML, et al. Among authors: noetzel mj. Bioorg Med Chem Lett. 2015 Mar 15;25(6):1310-7. doi: 10.1016/j.bmcl.2015.01.038. Epub 2015 Jan 28. Bioorg Med Chem Lett. 2015. PMID: 25683622 Free PMC article.
103 results