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Page 1
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
Gomtsyan A, Bayburt EK, Schmidt RG, Zheng GZ, Perner RJ, Didomenico S, Koenig JR, Turner S, Jinkerson T, Drizin I, Hannick SM, Macri BS, McDonald HA, Honore P, Wismer CT, Marsh KC, Wetter J, Stewart KD, Oie T, Jarvis MF, Surowy CS, Faltynek CR, Lee CH. Gomtsyan A, et al. Among authors: koenig jr. J Med Chem. 2005 Feb 10;48(3):744-52. doi: 10.1021/jm0492958. J Med Chem. 2005. PMID: 15689158
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.
Drizin I, Gomtsyan A, Bayburt EK, Schmidt RG, Zheng GZ, Perner RJ, DiDomenico S, Koenig JR, Turner SC, Jinkerson TK, Brown BS, Keddy RG, McDonald HA, Honore P, Wismer CT, Marsh KC, Wetter JM, Polakowski JS, Segreti JA, Jarvis MF, Faltynek CR, Lee CH. Drizin I, et al. Among authors: koenig jr. Bioorg Med Chem. 2006 Jul 15;14(14):4740-9. doi: 10.1016/j.bmc.2006.03.027. Epub 2006 Apr 18. Bioorg Med Chem. 2006. PMID: 16621571
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
Gomtsyan A, Bayburt EK, Keddy R, Turner SC, Jinkerson TK, Didomenico S, Perner RJ, Koenig JR, Drizin I, McDonald HA, Surowy CS, Honore P, Mikusa J, Marsh KC, Wetter JM, Faltynek CR, Lee CH. Gomtsyan A, et al. Among authors: koenig jr. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3894-9. doi: 10.1016/j.bmcl.2007.04.105. Epub 2007 May 3. Bioorg Med Chem Lett. 2007. PMID: 17507218
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
Perner RJ, DiDomenico S, Koenig JR, Gomtsyan A, Bayburt EK, Schmidt RG, Drizin I, Zheng GZ, Turner SC, Jinkerson T, Brown BS, Keddy RG, Lukin K, McDonald HA, Honore P, Mikusa J, Marsh KC, Wetter JM, George KS, Jarvis MF, Faltynek CR, Lee CH. Perner RJ, et al. Among authors: koenig jr. J Med Chem. 2007 Jul 26;50(15):3651-60. doi: 10.1021/jm070276i. Epub 2007 Jun 21. J Med Chem. 2007. PMID: 17583335
Discovery of TRPV1 antagonist ABT-116.
Brown BS, Keddy R, Perner RJ, DiDomenico S, Koenig JR, Jinkerson TK, Hannick SM, McDonald HA, Bianchi BR, Honore P, Puttfarcken PS, Moreland RB, Marsh KC, Faltynek CR, Lee CH. Brown BS, et al. Among authors: koenig jr. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3291-4. doi: 10.1016/j.bmcl.2010.04.047. Epub 2010 Apr 14. Bioorg Med Chem Lett. 2010. PMID: 20457518
Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists.
Schmidt RG, Bayburt EK, Latshaw SP, Koenig JR, Daanen JF, McDonald HA, Bianchi BR, Zhong C, Joshi S, Honore P, Marsh KC, Lee CH, Faltynek CR, Gomtsyan A. Schmidt RG, et al. Among authors: koenig jr. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1338-41. doi: 10.1016/j.bmcl.2011.01.056. Epub 2011 Jan 21. Bioorg Med Chem Lett. 2011. PMID: 21315587
Pyridopyrimidine analogues as novel adenosine kinase inhibitors.
Zheng GZ, Lee C, Pratt JK, Perner RJ, Jiang MQ, Gomtsyan A, Matulenko MA, Mao Y, Koenig JR, Kim KH, Muchmore S, Yu H, Kohlhaas K, Alexander KM, McGaraughty S, Chu KL, Wismer CT, Mikusa J, Jarvis MF, Marsh K, Kowaluk EA, Bhagwat SS, Stewart AO. Zheng GZ, et al. Among authors: koenig jr. Bioorg Med Chem Lett. 2001 Aug 20;11(16):2071-4. doi: 10.1016/s0960-894x(01)00375-4. Bioorg Med Chem Lett. 2001. PMID: 11514141
Adenosine kinase inhibitors: polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity.
Zheng GZ, Mao Y, Lee CH, Pratt JK, Koenig JR, Perner RJ, Cowart MD, Gfesser GA, McGaraughty S, Chu KL, Zhu C, Yu H, Kohlhaas K, Alexander KM, Wismer CT, Mikusa J, Jarvis MF, Kowaluk EA, Stewart AO. Zheng GZ, et al. Among authors: koenig jr. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3041-4. doi: 10.1016/s0960-894x(03)00642-5. Bioorg Med Chem Lett. 2003. PMID: 12941329
35 results