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Design and synthesis of potent, orally active, inhibitors of carboxypeptidase U (TAFIa).
Bioorg Med Chem. 2004 Mar 1;12(5):1151-75. doi: 10.1016/j.bmc.2003.12.039.
Bioorg Med Chem. 2004.
PMID: 14980627
Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that does not prolong bleeding.
Singh J, Zeller W, Zhou N, Hategan G, Mishra RK, Polozov A, Yu P, Onua E, Zhang J, Ramírez JL, Sigthorsson G, Thorsteinnsdottir M, Kiselyov AS, Zembower DE, Andrésson T, Gurney ME.
Singh J, et al. Among authors: hategan g.
J Med Chem. 2010 Jan 14;53(1):18-36. doi: 10.1021/jm9005912.
J Med Chem. 2010.
PMID: 19957930
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Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists.
Hategan G, Polozov AM, Zeller W, Cao H, Mishra RK, Kiselyov AS, Ramirez J, Halldorsdottir G, Andrésson T, Gurney ME, Singh J.
Hategan G, et al.
Bioorg Med Chem Lett. 2009 Dec 1;19(23):6797-800. doi: 10.1016/j.bmcl.2009.09.084. Epub 2009 Sep 27.
Bioorg Med Chem Lett. 2009.
PMID: 19836233
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