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Page 1
Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.
Tang H, Zhu Y, Teumelsan N, Walsh SP, Shahripour A, Priest BT, Swensen AM, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Pai LY, Hampton C, Corona A, Hernandez M, Metzger J, Forrest M, Zhou X, Owens K, Tong V, Parmee E, Roy S, Kaczorowski GJ, Yang L, Alonso-Galicia M, Garcia ML, Pasternak A. Tang H, et al. Among authors: kaczorowski gj. ACS Med Chem Lett. 2016 May 12;7(7):697-701. doi: 10.1021/acsmedchemlett.6b00122. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437080 Free PMC article.
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: kaczorowski gj. 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. Among authors: kaczorowski gj. 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.
Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.
Walsh SP, Shahripour A, Tang H, Teumelsan N, Frie J, Zhu Y, Priest BT, Swensen AM, Liu J, Margulis M, Visconti R, Weinglass A, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Alonso-Galicia M, Zhou X, Pai LY, Corona A, Hampton C, Hernandez M, Bentley R, Chen J, Shah K, Metzger J, Forrest M, Owens K, Tong V, Ha S, Roy S, Kaczorowski GJ, Yang L, Parmee E, Garcia ML, Sullivan K, Pasternak A. Walsh SP, et al. Among authors: kaczorowski gj. ACS Med Chem Lett. 2015 May 7;6(7):747-52. doi: 10.1021/ml500440u. eCollection 2015 Jul 9. ACS Med Chem Lett. 2015. PMID: 26191360 Free PMC article.
Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation.
Walsh SP, Shahripour A, Tang H, de Jesus RK, Teumelsan N, Zhu Y, Frie J, 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, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Garcia ML, Pasternak A. Walsh SP, et al. Among authors: kaczorowski gj. Bioorg Med Chem Lett. 2016 May 1;26(9):2339-43. doi: 10.1016/j.bmcl.2016.03.035. Epub 2016 Mar 12. Bioorg Med Chem Lett. 2016. PMID: 27017115
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.
Zhu Y, de Jesus RK, Tang H, Walsh SP, Jiang J, Gu X, Teumelsan N, Shahripour A, Pio B, Ding FX, Ha S, 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, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Parmee ER, Sullivan K, Garcia ML, Pasternak A. Zhu Y, et al. Among authors: kaczorowski gj. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5695-5702. doi: 10.1016/j.bmcl.2016.10.064. Epub 2016 Oct 24. Bioorg Med Chem Lett. 2016. PMID: 27839686
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: kaczorowski gj. 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
Synthesis and SAR of 1,2-trans-(1-hydroxy-3-phenylprop-1-yl)cyclopentane carboxamide derivatives, a new class of sodium channel blockers.
Ok D, Li C, Abbadie C, Felix JP, Fisher MH, Garcia ML, Kaczorowski GJ, Lyons KA, Martin WJ, Priest BT, Smith MM, Williams BS, Wyvratt MJ, Parsons WH. Ok D, et al. Among authors: kaczorowski gj. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1358-61. doi: 10.1016/j.bmcl.2005.11.051. Epub 2005 Dec 5. Bioorg Med Chem Lett. 2006. PMID: 16337121
The inwardly rectifying potassium channel Kir1.1: development of functional assays to identify and characterize channel inhibitors.
Felix JP, Priest BT, Solly K, Bailey T, Brochu RM, Liu CJ, Kohler MG, Kiss L, Alonso-Galicia M, Tang H, Pasternak A, Kaczorowski GJ, Garcia ML. Felix JP, et al. Among authors: kaczorowski gj. Assay Drug Dev Technol. 2012 Oct;10(5):417-31. doi: 10.1089/adt.2012.462. Epub 2012 Aug 10. Assay Drug Dev Technol. 2012. PMID: 22881347
A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic pain.
Hoyt SB, London C, Abbadie C, Felix JP, Garcia ML, Jochnowitz N, Karanam BV, Li X, Lyons KA, McGowan E, Priest BT, Smith MM, Warren VA, Thomas-Fowlkes BS, Kaczorowski GJ, Duffy JL. Hoyt SB, et al. Among authors: kaczorowski gj. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3640-5. doi: 10.1016/j.bmcl.2013.03.121. Epub 2013 Apr 5. Bioorg Med Chem Lett. 2013. PMID: 23652221
181 results