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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: macdonald sjf. 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
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: macdonald sjf. 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 and Development of Highly Potent and Orally Bioavailable Nonpeptidic αvβ6 Integrin Inhibitors.
Procopiou PA, Barrett J, Crawford MHJ, Hatley RJD, Hancock AP, Pritchard JM, Rowedder JE, Copley RCB, Slack RJ, Sollis SL, Thorp LR, Lippa RA, Macdonald SJF, Barrett TN. Procopiou PA, et al. Among authors: macdonald sjf. J Med Chem. 2024 Oct 10;67(19):17497-17519. doi: 10.1021/acs.jmedchem.4c01430. Epub 2024 Sep 13. J Med Chem. 2024. PMID: 39269712
Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhibitors.
Schwehm C, Kellam B, Garces AE, Hill SJ, Kindon ND, Bradshaw TD, Li J, Macdonald SJ, Rowedder JE, Stoddart LA, Stocks MJ. Schwehm C, et al. J Med Chem. 2017 Feb 23;60(4):1534-1554. doi: 10.1021/acs.jmedchem.6b01801. Epub 2017 Feb 10. J Med Chem. 2017. PMID: 28128944 Free article.
Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of N-Methylation for PI3Kδ Activity.
Barnes L, Blaber H, Brooks DTK, Byers L, Buckley D, Byron ZC, Chilvers RG, Cochrane L, Cooney E, Damian HA, Francis L, Fu He D, Grace JMJ, Green HJ, Hogarth EJP, Jusu L, Killalea CE, King O, Lambert J, Lee ZJ, Lima NS, Long CL, Mackinnon ML, Mahdy S, Matthews-Wright J, Millward MJ, Meehan MF, Merrett C, Morrison L, Parke HRI, Payne C, Payne L, Pike C, Seal A, Senior AJ, Smith KM, Stanelyte K, Stillibrand J, Szpara R, Taday FFH, Threadgould AM, Trainor RJ, Waters J, Williams O, Wong CKW, Wood K, Barton N, Gruszka A, Henley Z, Rowedder JE, Cookson R, Jones KL, Nadin A, Smith IE, Macdonald SJF, Nortcliffe A. Barnes L, et al. Among authors: macdonald sjf. J Med Chem. 2019 Nov 27;62(22):10402-10422. doi: 10.1021/acs.jmedchem.9b01499. Epub 2019 Nov 6. J Med Chem. 2019. PMID: 31647659
82 results