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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: 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.
Emergence of Small-Molecule Non-RGD-Mimetic Inhibitors for RGD Integrins.
Miller LM, Pritchard JM, Macdonald SJF, Jamieson C, Watson AJB. Miller LM, et al. Among authors: macdonald sjf. J Med Chem. 2017 Apr 27;60(8):3241-3251. doi: 10.1021/acs.jmedchem.6b01711. Epub 2017 Feb 15. J Med Chem. 2017. PMID: 28135089 Free article. Review.
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
Structure Activity Relationships of αv Integrin Antagonists for Pulmonary Fibrosis by Variation in Aryl Substituents.
Adams J, Anderson EC, Blackham EE, Chiu YW, Clarke T, Eccles N, Gill LA, Haye JJ, Haywood HT, Hoenig CR, Kausas M, Le J, Russell HL, Smedley C, Tipping WJ, Tongue T, Wood CC, Yeung J, Rowedder JE, Fray MJ, McInally T, Macdonald SJ. Adams J, et al. ACS Med Chem Lett. 2014 Sep 19;5(11):1207-12. doi: 10.1021/ml5002079. eCollection 2014 Nov 13. ACS Med Chem Lett. 2014. PMID: 25408832 Free PMC article.
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.
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