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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: didomenico s. J Med Chem. 2005 Feb 10;48(3):744-52. doi: 10.1021/jm0492958. J Med Chem. 2005. PMID: 15689158
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: didomenico s. Bioorg Med Chem. 2005 Jun 1;13(11):3705-20. doi: 10.1016/j.bmc.2005.03.023. Bioorg Med Chem. 2005. PMID: 15863000
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: didomenico s. 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
4-amino-5-aryl-6-arylethynylpyrimidines: structure-activity relationships of non-nucleoside adenosine kinase inhibitors.
Matulenko MA, Paight ES, Frey RR, Gomtsyan A, DiDomenico S Jr, Jiang M, Lee CH, Stewart AO, Yu H, Kohlhaas KL, Alexander KM, McGaraughty S, Mikusa J, Marsh KC, Muchmore SW, Jakob CL, Kowaluk EA, Jarvis MF, Bhagwat SS. Matulenko MA, et al. Among authors: didomenico s jr. Bioorg Med Chem. 2007 Feb 15;15(4):1586-605. doi: 10.1016/j.bmc.2006.12.029. Epub 2006 Dec 20. Bioorg Med Chem. 2007. PMID: 17197188
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: didomenico s. 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: didomenico s. J Med Chem. 2007 Jul 26;50(15):3651-60. doi: 10.1021/jm070276i. Epub 2007 Jun 21. J Med Chem. 2007. PMID: 17583335
22 results