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Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs.
Davis DC, Bungard JD, Chang S, Rodriguez AL, Blobaum AL, Boutaud O, Melancon BJ, Niswender CM, Jeffrey Conn P, Lindsley CW. Davis DC, et al. Among authors: lindsley cw. Bioorg Med Chem Lett. 2021 Jan 15;32:127724. doi: 10.1016/j.bmcl.2020.127724. Epub 2020 Nov 27. Bioorg Med Chem Lett. 2021. PMID: 33253881
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL Jr, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR. Lindsley CW, et al. J Med Chem. 2004 Nov 18;47(24):5825-8. doi: 10.1021/jm049400d. J Med Chem. 2004. PMID: 15537338
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Wittman M, Ha SN, Schaffhauser H, Sur C, Pettibone DJ, Duggan ME, Conn PJ, Hartman GD, Lindsley CW. Zhao Z, et al. Among authors: lindsley cw. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1386-91. doi: 10.1016/j.bmcl.2006.11.081. Epub 2006 Dec 3. Bioorg Med Chem Lett. 2007. PMID: 17210250
Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.
Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, Williams R, Lindsley CW, Conn PJ. Niswender CM, et al. Among authors: lindsley cw. Mol Pharmacol. 2008 Nov;74(5):1345-58. doi: 10.1124/mol.108.049551. Epub 2008 Jul 29. Mol Pharmacol. 2008. PMID: 18664603 Free PMC article.
Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators.
Niswender CM, Lebois EP, Luo Q, Kim K, Muchalski H, Yin H, Conn PJ, Lindsley CW. Niswender CM, et al. Among authors: lindsley cw. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5626-30. doi: 10.1016/j.bmcl.2008.08.087. Epub 2008 Aug 29. Bioorg Med Chem Lett. 2008. PMID: 18793851 Free PMC article.
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
Bridges TM, Brady AE, Kennedy JP, Daniels RN, Miller NR, Kim K, Breininger ML, Gentry PR, Brogan JT, Jones CK, Conn PJ, Lindsley CW. Bridges TM, et al. Among authors: lindsley cw. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5439-42. doi: 10.1016/j.bmcl.2008.09.023. Epub 2008 Sep 10. Bioorg Med Chem Lett. 2008. PMID: 18805692 Free PMC article.
746 results