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Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase.
Levell J, Astles P, Eastwood P, Cairns J, Houille O, Aldous S, Merriman G, Whiteley B, Pribish J, Czekaj M, Liang G, Maignan S, Guilloteau JP, Dupuy A, Davidson J, Harrison T, Morley A, Watson S, Fenton G, McCarthy C, Romano J, Mathew R, Engers D, Gardyan M, Sides K, Kwong J, Tsay J, Rebello S, Shen L, Wang J, Luo Y, Giardino O, Lim HK, Smith K, Pauls H. Levell J, et al. Among authors: engers d. Bioorg Med Chem. 2005 Apr 15;13(8):2859-72. doi: 10.1016/j.bmc.2005.02.014. Bioorg Med Chem. 2005. PMID: 15781396
Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M4 muscarinic acetylcholine receptor.
Bender AM, Carter TR, Spock M, Rodriguez AL, Dickerson JW, Rook JM, Chang S, Qi A, Presley CC, Engers DW, Harp JM, Bridges TM, Niswender CM, Conn PJ, Lindsley CW. Bender AM, et al. Among authors: engers dw. Bioorg Med Chem Lett. 2022 Jan 15;56:128479. doi: 10.1016/j.bmcl.2021.128479. Epub 2021 Nov 24. Bioorg Med Chem Lett. 2022. PMID: 34838649
Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter.
Bollinger SR, Engers DW, Ennis EA, Wright J, Locuson CW, Lindsley CW, Blakely RD, Hopkins CR. Bollinger SR, et al. Among authors: engers dw. Bioorg Med Chem Lett. 2015 Apr 15;25(8):1757-1760. doi: 10.1016/j.bmcl.2015.02.058. Epub 2015 Feb 28. Bioorg Med Chem Lett. 2015. PMID: 25801932 Free PMC article.
The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core.
Bertron JL, Cho HP, Garcia-Barrantes PM, Panarese JD, Salovich JM, Nance KD, Engers DW, Rook JM, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW. Bertron JL, et al. Among authors: engers dw. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2175-2179. doi: 10.1016/j.bmcl.2018.05.009. Epub 2018 May 5. Bioorg Med Chem Lett. 2018. PMID: 29754948 Free PMC article.
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. 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.
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. 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.
Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1.
Spearing PK, Cho HP, Luscombe VB, Blobaum AL, Boutaud O, Engers DW, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Bender AM. Spearing PK, et al. Among authors: engers dw. Bioorg Med Chem Lett. 2021 Sep 1;47:128193. doi: 10.1016/j.bmcl.2021.128193. Epub 2021 Jun 9. Bioorg Med Chem Lett. 2021. PMID: 34118412 Free PMC article.
Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes - Part 2.
Long MF, Capstick RA, Spearing PK, Engers JL, Gregro AR, Bollinger SR, Chang S, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Lindsley CW, Engers DW, Temple KJ. Long MF, et al. Among authors: engers dw. Bioorg Med Chem Lett. 2021 Dec 1;53:128416. doi: 10.1016/j.bmcl.2021.128416. Epub 2021 Oct 26. Bioorg Med Chem Lett. 2021. PMID: 34710625 Free PMC article.
Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Engers DW, Frist AY, Lindsley CW, Hong CC, Hopkins CR. Engers DW, et al. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52. doi: 10.1016/j.bmcl.2013.03.113. Epub 2013 Apr 11. Bioorg Med Chem Lett. 2013. PMID: 23639540 Free PMC article.
84 results