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Page 1
Substituted biaryl pyrazoles as sodium channel blockers.
Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Fisher MH, Wyvratt MJ, Lyons K, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Parsons WH. Tyagarajan S, et al. Among authors: brochu rm. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5480-3. doi: 10.1016/j.bmcl.2010.07.080. Epub 2010 Jul 24. Bioorg Med Chem Lett. 2010. PMID: 20709545
A disubstituted succinamide is a potent sodium channel blocker with efficacy in a rat pain model.
Priest BT, Garcia ML, Middleton RE, Brochu RM, Clark S, Dai G, Dick IE, Felix JP, Liu CJ, Reiseter BS, Schmalhofer WA, Shao PP, Tang YS, Chou MZ, Kohler MG, Smith MM, Warren VA, Williams BS, Cohen CJ, Martin WJ, Meinke PT, Parsons WH, Wafford KA, Kaczorowski GJ. Priest BT, et al. Among authors: brochu rm. Biochemistry. 2004 Aug 3;43(30):9866-76. doi: 10.1021/bi0493259. Biochemistry. 2004. PMID: 15274641
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.
Liang J, Brochu RM, Cohen CJ, Dick IE, Felix JP, Fisher MH, Garcia ML, Kaczorowski GJ, Lyons KA, Meinke PT, Priest BT, Schmalhofer WA, Smith MM, Tarpley JW, Williams BS, Martin WJ, Parsons WH. Liang J, et al. Among authors: brochu rm. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2943-7. doi: 10.1016/j.bmcl.2005.02.093. Bioorg Med Chem Lett. 2005. PMID: 15878274
Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers.
Tyagarajan S, Chakravarty PK, Zhou B, Fisher MH, Wyvratt MJ, Lyons K, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Parsons WH. Tyagarajan S, et al. Among authors: brochu rm. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5536-40. doi: 10.1016/j.bmcl.2010.07.064. Epub 2010 Jul 21. Bioorg Med Chem Lett. 2010. PMID: 20709552
Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.
Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Eid R, Fisher MH, Parsons WH, Wyvratt MJ, Lyons KA, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Weber A, Duffy JL. Tyagarajan S, et al. Among authors: brochu rm. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7479-82. doi: 10.1016/j.bmcl.2010.10.017. Epub 2010 Oct 14. Bioorg Med Chem Lett. 2010. PMID: 21106456
Discovery of a novel sub-class of ROMK channel inhibitors typified by 5-(2-(4-(2-(4-(1H-Tetrazol-1-yl)phenyl)acetyl)piperazin-1-yl)ethyl)isobenzofuran-1(3H)-one.
Tang H, de Jesus RK, Walsh SP, Zhu Y, Yan Y, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Roy S, Kaczorowski GJ, Yang L, Garcia ML, Pasternak A. Tang H, et al. Among authors: brochu rm. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5829-32. doi: 10.1016/j.bmcl.2013.08.104. Epub 2013 Sep 6. Bioorg Med Chem Lett. 2013. PMID: 24075732
Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics.
Tang H, Walsh SP, Yan Y, de Jesus RK, Shahripour A, Teumelsan N, Zhu Y, Ha S, Owens KA, Thomas-Fowlkes BS, Felix JP, Liu J, Kohler M, Priest BT, Bailey T, Brochu R, Alonso-Galicia M, Kaczorowski GJ, Roy S, Yang L, Mills SG, Garcia ML, Pasternak A. Tang H, et al. ACS Med Chem Lett. 2012 Mar 28;3(5):367-72. doi: 10.1021/ml3000066. eCollection 2012 May 10. ACS Med Chem Lett. 2012. PMID: 24900480 Free PMC article.
30 results