Costanzo MJ - Search Results

1

In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.

Costanzo MJ, Almond HR Jr, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Corcoran TW, Giardino EC, Kauffman JA, Lewis JM, de Garavilla L, Haertlein BJ, Maryanoff BE. Costanzo MJ, et al. J Med Chem. 2005 Mar 24;48(6):1984-2008. doi: 10.1021/jm0303857. J Med Chem. 2005. PMID: 15771442

2

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. J Med Chem. 2003 Aug 28;46(18):3865-76. doi: 10.1021/jm030050p. J Med Chem. 2003. PMID: 12930148

3

Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform.

Maryanoff BE, McComsey DF, Costanzo MJ, Hochman C, Smith-Swintosky V, Shank RP. Maryanoff BE, et al. Among authors: costanzo mj. J Med Chem. 2005 Mar 24;48(6):1941-7. doi: 10.1021/jm040124c. J Med Chem. 2005. PMID: 15771438

4

Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.

Maryanoff BE, Costanzo MJ. Maryanoff BE, et al. Among authors: costanzo mj. Bioorg Med Chem. 2008 Feb 15;16(4):1562-95. doi: 10.1016/j.bmc.2007.11.015. Epub 2007 Nov 6. Bioorg Med Chem. 2008. PMID: 18053726 Review.

5

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. 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

6

Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group.

Costanzo MJ, Maryanoff BE, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Kauffman JA, Lewis JM, Krishnan R, Tulinsky A. Costanzo MJ, et al. J Med Chem. 1996 Aug 2;39(16):3039-43. doi: 10.1021/jm9603274. J Med Chem. 1996. PMID: 8759623 No abstract available.

7

Structure-activity studies on anticonvulsant sugar sulfamates related to topiramate. Enhanced potency with cyclic sulfate derivatives.

Maryanoff BE, Costanzo MJ, Nortey SO, Greco MN, Shank RP, Schupsky JJ, Ortegon MP, Vaught JL. Maryanoff BE, et al. Among authors: costanzo mj. J Med Chem. 1998 Apr 9;41(8):1315-43. doi: 10.1021/jm970790w. J Med Chem. 1998. PMID: 9548821

8

Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.

Hoekstra WJ, Maryanoff BE, Damiano BP, Andrade-Gordon P, Cohen JH, Costanzo MJ, Haertlein BJ, Hecker LR, Hulshizer BL, Kauffman JA, Keane P, McComsey DF, Mitchell JA, Scott L, Shah RD, Yabut SC. Hoekstra WJ, et al. Among authors: costanzo mj. J Med Chem. 1999 Dec 16;42(25):5254-65. doi: 10.1021/jm990418b. J Med Chem. 1999. PMID: 10602710

9

Antithrombotic properties of RWJ-50353, a potent and novel thrombin inhibitor.

Giardino EC, Costanzo MJ, Kauffman JA, Li QS, Maryanoff BE, Andrade-Gordon P. Giardino EC, et al. Among authors: costanzo mj. Thromb Res. 2000 Apr 1;98(1):83-93. doi: 10.1016/s0049-3848(99)00219-4. Thromb Res. 2000. PMID: 10706936

10

Exploration of potential prodrugs of RWJ-445167, an oxyguanidine-based dual inhibitor of thrombin and factor Xa.

Maryanoff BE, McComsey DF, Costanzo MJ, Yabut SC, Lu T, Player MR, Giardino EC, Damiano BP. Maryanoff BE, et al. Among authors: costanzo mj. Chem Biol Drug Des. 2006 Jul;68(1):29-36. doi: 10.1111/j.1747-0285.2006.00408.x. Chem Biol Drug Des. 2006. PMID: 16923023

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