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Profile of a Highly Selective Quaternized Pyrrolidine Betaine αvβ6 Integrin Inhibitor-(3S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((1S and 1R,3R)-1-methyl-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-ium-1-yl)butanoate Synthesized by Stereoselective Methylation.
Barrett TN, Taylor JA, Barker D, Procopiou PA, Thompson JDF, Barrett J, Le J, Lynn SM, Pogany P, Pratley C, Pritchard JM, Roper JA, Rowedder JE, Slack RJ, Vitulli G, Macdonald SJF, Kerr WJ. Barrett TN, et al. Among authors: vitulli g. J Med Chem. 2019 Aug 22;62(16):7543-7556. doi: 10.1021/acs.jmedchem.9b00819. Epub 2019 Aug 5. J Med Chem. 2019. PMID: 31381331 Free article.
Discovery of ( S)-3-(3-(3,5-Dimethyl-1 H-pyrazol-1-yl)phenyl)-4-(( R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis.
Procopiou PA, Anderson NA, Barrett J, Barrett TN, Crawford MHJ, Fallon BJ, Hancock AP, Le J, Lemma S, Marshall RP, Morrell J, Pritchard JM, Rowedder JE, Saklatvala P, Slack RJ, Sollis SL, Suckling CJ, Thorp LR, Vitulli G, Macdonald SJF. Procopiou PA, et al. Among authors: vitulli g. J Med Chem. 2018 Sep 27;61(18):8417-8443. doi: 10.1021/acs.jmedchem.8b00959. Epub 2018 Sep 14. J Med Chem. 2018. PMID: 30215258
Translational pharmacology of an inhaled small molecule αvβ6 integrin inhibitor for idiopathic pulmonary fibrosis.
John AE, Graves RH, Pun KT, Vitulli G, Forty EJ, Mercer PF, Morrell JL, Barrett JW, Rogers RF, Hafeji M, Bibby LI, Gower E, Morrison VS, Man Y, Roper JA, Luckett JC, Borthwick LA, Barksby BS, Burgoyne RA, Barnes R, Le J, Flint DJ, Pyne S, Habgood A, Organ LA, Joseph C, Edwards-Pritchard RC, Maher TM, Fisher AJ, Gudmann NS, Leeming DJ, Chambers RC, Lukey PT, Marshall RP, Macdonald SJF, Jenkins RG, Slack RJ. John AE, et al. Among authors: vitulli g. Nat Commun. 2020 Sep 16;11(1):4659. doi: 10.1038/s41467-020-18397-6. Nat Commun. 2020. PMID: 32938936 Free PMC article.
Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.
Down K, Amour A, Baldwin IR, Cooper AW, Deakin AM, Felton LM, Guntrip SB, Hardy C, Harrison ZA, Jones KL, Jones P, Keeling SE, Le J, Livia S, Lucas F, Lunniss CJ, Parr NJ, Robinson E, Rowland P, Smith S, Thomas DA, Vitulli G, Washio Y, Hamblin JN. Down K, et al. Among authors: vitulli g. J Med Chem. 2015 Sep 24;58(18):7381-99. doi: 10.1021/acs.jmedchem.5b00767. Epub 2015 Sep 3. J Med Chem. 2015. PMID: 26301626
Preclinical evaluation of [18F]FB-A20FMDV2 as a selective marker for measuring αVβ6 integrin occupancy using positron emission tomography in rodent lung.
Onega M, Parker CA, Coello C, Rizzo G, Keat N, Ramada-Magalhaes J, Moz S, Tang SP, Plisson C, Wells L, Ashworth S, Slack RJ, Vitulli G, Wilson FJ, Gunn R, Lukey PT, Passchier J. Onega M, et al. Among authors: vitulli g. Eur J Nucl Med Mol Imaging. 2020 Apr;47(4):958-966. doi: 10.1007/s00259-019-04653-5. Epub 2020 Jan 3. Eur J Nucl Med Mol Imaging. 2020. PMID: 31897589 Free PMC article.
Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.
Amour A, Barton N, Cooper AW, Inglis G, Jamieson C, Luscombe CN, Morrell J, Peace S, Perez D, Rowland P, Tame CJ, Uddin S, Vitulli G, Wellaway N. Amour A, et al. Among authors: vitulli g. J Med Chem. 2016 Aug 11;59(15):7239-51. doi: 10.1021/acs.jmedchem.6b00799. Epub 2016 Jul 27. J Med Chem. 2016. PMID: 27429068 Free article.
Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists.
Micheli F, Fabio RD, Cavanni P, Rimland JM, Capelli AM, Chiamulera C, Corsi M, Corti C, Donati D, Feriani A, Ferraguti F, Maffeis M, Missio A, Ratti E, Paio A, Pachera R, Quartaroli M, Reggiani A, Sabbatini FM, Trist DG, Ugolini A, Vitulli G. Micheli F, et al. Among authors: vitulli g. Bioorg Med Chem. 2003 Jan 17;11(2):171-83. doi: 10.1016/s0968-0896(02)00424-8. Bioorg Med Chem. 2003. PMID: 12470711
29 results