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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: sides k. Bioorg Med Chem. 2005 Apr 15;13(8):2859-72. doi: 10.1016/j.bmc.2005.02.014. Bioorg Med Chem. 2005. PMID: 15781396
Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.
Hopkins C, Neuenschwander K, Scotese A, Jackson S, Nieduzak T, Pauls H, Liang G, Sides K, Cramer D, Cairns J, Maignan S, Mathieu M. Hopkins C, et al. Among authors: sides k. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4819-23. doi: 10.1016/j.bmcl.2004.07.051. Bioorg Med Chem Lett. 2004. PMID: 15341931
Design of bivalent ligands using hydrogen bond linkers: synthesis and evaluation of inhibitors for human beta-tryptase.
Vaz RJ, Gao Z, Pribish J, Chen X, Levell J, Davis L, Albert E, Brollo M, Ugolini A, Cramer DM, Cairns J, Sides K, Liu F, Kwong J, Kang J, Rebello S, Elliot M, Lim H, Chellaraj V, Singleton RW, Li Y. Vaz RJ, et al. Among authors: sides k. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6053-6. doi: 10.1016/j.bmcl.2004.09.065. Bioorg Med Chem Lett. 2004. PMID: 15546728
A conformationally constrained inhibitor with an enhanced potency for β-tryptase and stability against semicarbazide-sensitive amine oxidase (SSAO).
Liang G, Choi-Sledeski YM, Poli G, Chen X, Shum P, Minnich A, Wang Q, Tsay J, Sides K, Cairns J, Stoklosa G, Nieduzak T, Zhao Z, Wang J, Vaz RJ. Liang G, et al. Among authors: sides k. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6721-4. doi: 10.1016/j.bmcl.2010.08.141. Epub 2010 Sep 6. Bioorg Med Chem Lett. 2010. PMID: 20855210
Structure-based library design and the discovery of a potent and selective mast cell β-tryptase inhibitor as an oral therapeutic agent.
Liang G, Aldous S, Merriman G, Levell J, Pribish J, Cairns J, Chen X, Maignan S, Mathieu M, Tsay J, Sides K, Rebello S, Whitely B, Morize I, Pauls HW. Liang G, et al. Among authors: sides k. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1049-54. doi: 10.1016/j.bmcl.2011.11.119. Epub 2011 Dec 7. Bioorg Med Chem Lett. 2012. PMID: 22192588
16 results