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Potency variation of small-molecule chymase inhibitors across species.
Kervinen J, Crysler C, Bayoumy S, Abad MC, Spurlino J, Deckman I, Greco MN, Maryanoff BE, de Garavilla L. Kervinen J, et al. Among authors: maryanoff be. Biochem Pharmacol. 2010 Oct 1;80(7):1033-41. doi: 10.1016/j.bcp.2010.06.014. Epub 2010 Jun 23. Biochem Pharmacol. 2010. PMID: 20599788
Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.
Costanzo MJ, Yabut SC, Almond HR Jr, Andrade-Gordon P, Corcoran TW, De Garavilla L, Kauffman JA, Abraham WM, Recacha R, Chattopadhyay D, Maryanoff BE. Costanzo MJ, et al. Among authors: maryanoff be. J Med Chem. 2003 Aug 28;46(18):3865-76. doi: 10.1021/jm030050p. J Med Chem. 2003. PMID: 12930148
A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.
de Garavilla L, Greco MN, Sukumar N, Chen ZW, Pineda AO, Mathews FS, Di Cera E, Giardino EC, Wells GI, Haertlein BJ, Kauffman JA, Corcoran TW, Derian CK, Eckardt AJ, Damiano BP, Andrade-Gordon P, Maryanoff BE. de Garavilla L, et al. Among authors: maryanoff be. J Biol Chem. 2005 May 6;280(18):18001-7. doi: 10.1074/jbc.M501302200. Epub 2005 Feb 28. J Biol Chem. 2005. PMID: 15741158 Free article.
Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives.
Costanzo MJ, Yabut SC, Zhang HC, White KB, de Garavilla L, Wang Y, Minor LK, Tounge BA, Barnakov AN, Lewandowski F, Milligan C, Spurlino JC, Abraham WM, Boswell-Smith V, Page CP, Maryanoff BE. Costanzo MJ, et al. Among authors: maryanoff be. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2114-21. doi: 10.1016/j.bmcl.2008.01.093. Epub 2008 Jan 30. Bioorg Med Chem Lett. 2008. PMID: 18272363
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.
Lu T, Markotan T, Ballentine SK, Giardino EC, Spurlino J, Crysler CS, Brown K, Maryanoff BE, Tomczuk BE, Damiano BP, Shukla U, End D, Andrade-Gordon P, Bone RF, Player MR. Lu T, et al. Among authors: maryanoff be. J Med Chem. 2010 Feb 25;53(4):1843-56. doi: 10.1021/jm901802n. J Med Chem. 2010. PMID: 20102150 Clinical Trial.
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
Lee YK, Parks DJ, Lu T, Thieu TV, Markotan T, Pan W, McComsey DF, Milkiewicz KL, Crysler CS, Ninan N, Abad MC, Giardino EC, Maryanoff BE, Damiano BP, Player MR. Lee YK, et al. Among authors: maryanoff be. J Med Chem. 2008 Jan 24;51(2):282-97. doi: 10.1021/jm701217r. Epub 2007 Dec 27. J Med Chem. 2008. PMID: 18159923
140 results