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1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D4 Receptor.
Del Bello F, Bonifazi A, Giorgioni G, Cifani C, Micioni Di Bonaventura MV, Petrelli R, Piergentili A, Fontana S, Mammoli V, Yano H, Matucci R, Vistoli G, Quaglia W. Del Bello F, et al. Among authors: matucci r. J Med Chem. 2018 Apr 26;61(8):3712-3725. doi: 10.1021/acs.jmedchem.8b00265. Epub 2018 Apr 6. J Med Chem. 2018. PMID: 29589445
Novel Potent Muscarinic Receptor Antagonists: Investigation on the Nature of Lipophilic Substituents in the 5- and/or 6-Positions of the 1,4-Dioxane Nucleus.
Del Bello F, Bonifazi A, Giorgioni G, Piergentili A, Sabbieti MG, Agas D, Dell'Aera M, Matucci R, Górecki M, Pescitelli G, Vistoli G, Quaglia W. Del Bello F, et al. Among authors: matucci r. J Med Chem. 2020 Jun 11;63(11):5763-5782. doi: 10.1021/acs.jmedchem.9b02100. Epub 2020 May 19. J Med Chem. 2020. PMID: 32374602 Free PMC article.
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
Bonifazi A, Yano H, Del Bello F, Farande A, Quaglia W, Petrelli R, Matucci R, Nesi M, Vistoli G, Ferré S, Piergentili A. Bonifazi A, et al. Among authors: matucci r. J Med Chem. 2014 Nov 13;57(21):9065-77. doi: 10.1021/jm501173q. Epub 2014 Oct 16. J Med Chem. 2014. PMID: 25275964
The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT1A receptor over α1-adrenoceptor and D2-like receptor subtypes.
Del Bello F, Bonifazi A, Giannella M, Giorgioni G, Piergentili A, Petrelli R, Cifani C, Micioni Di Bonaventura MV, Keck TM, Mazzolari A, Vistoli G, Cilia A, Poggesi E, Matucci R, Quaglia W. Del Bello F, et al. Among authors: matucci r. Eur J Med Chem. 2017 Jan 5;125:233-244. doi: 10.1016/j.ejmech.2016.09.026. Epub 2016 Sep 9. Eur J Med Chem. 2017. PMID: 27662034
80 results