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Page 1
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: lee ch. 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
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: lee ch. 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
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: lee ch. J Med Chem. 2005 Feb 10;48(3):744-52. doi: 10.1021/jm0492958. J Med Chem. 2005. PMID: 15689158
A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats.
Honore P, Wismer CT, Mikusa J, Zhu CZ, Zhong C, Gauvin DM, Gomtsyan A, El Kouhen R, Lee CH, Marsh K, Sullivan JP, Faltynek CR, Jarvis MF. Honore P, et al. Among authors: lee ch. J Pharmacol Exp Ther. 2005 Jul;314(1):410-21. doi: 10.1124/jpet.105.083915. Epub 2005 Apr 18. J Pharmacol Exp Ther. 2005. PMID: 15837818
A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid.
El Kouhen R, Surowy CS, Bianchi BR, Neelands TR, McDonald HA, Niforatos W, Gomtsyan A, Lee CH, Honore P, Sullivan JP, Jarvis MF, Faltynek CR. El Kouhen R, et al. Among authors: lee ch. J Pharmacol Exp Ther. 2005 Jul;314(1):400-9. doi: 10.1124/jpet.105.084103. Epub 2005 Apr 18. J Pharmacol Exp Ther. 2005. PMID: 15837819
5-(3-Bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine: structure-activity relationships of 7-substituted heteroaryl analogs as non-nucleoside adenosine kinase inhibitors.
Matulenko MA, Lee CH, Jiang M, Frey RR, Cowart MD, Bayburt EK, Didomenico S, Gfesser GA, Gomtsyan A, Zheng GZ, McKie JA, Stewart AO, Yu H, Kohlhaas KL, Alexander KM, McGaraughty S, Wismer CT, Mikusa J, Marsh KC, Snyder RD, Diehl MS, Kowaluk EA, Jarvis MF, Bhagwat SS. Matulenko MA, et al. Among authors: lee ch. Bioorg Med Chem. 2005 Jun 1;13(11):3705-20. doi: 10.1016/j.bmc.2005.03.023. Bioorg Med Chem. 2005. PMID: 15863000
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