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Page 1
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: roy s. 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 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: roy s. 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 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: roy s. 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: roy s. 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 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: roy s. 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 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: roy s. 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
Pharmacologic inhibition of the renal outer medullary potassium channel causes diuresis and natriuresis in the absence of kaliuresis.
Garcia ML, Priest BT, Alonso-Galicia M, Zhou X, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Liu J, Swensen A, Pai LY, Xiao J, Hernandez M, Hoagland K, Owens K, Tang H, de Jesus RK, Roy S, Kaczorowski GJ, Pasternak A. Garcia ML, et al. Among authors: roy s. J Pharmacol Exp Ther. 2014 Jan;348(1):153-64. doi: 10.1124/jpet.113.208603. Epub 2013 Oct 18. J Pharmacol Exp Ther. 2014. PMID: 24142912
The Renal Outer Medullary Potassium Channel Inhibitor, MK-7145, Lowers Blood Pressure, and Manifests Features of Bartter's Syndrome Type II Phenotype.
Hampton C, Zhou X, Priest BT, Pai LY, Felix JP, Thomas-Fowlkes B, Liu J, Kohler M, Xiao J, Corona A, Price O, Gill C, Shah K, Rasa C, Tong V, Owens K, Ormes J, Tang H, Roy S, Sullivan KA, Metzger JM, Alonso-Galicia M, Kaczorowski GJ, Pasternak A, Garcia ML. Hampton C, et al. Among authors: roy s. J Pharmacol Exp Ther. 2016 Oct;359(1):194-206. doi: 10.1124/jpet.116.235150. Epub 2016 Jul 18. J Pharmacol Exp Ther. 2016. PMID: 27432892
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.
Dong S, VanGelder K, Shi ZC, Yu Y, Wu Z, Ferguson R, Guo ZZ, Tang H, Frie J, Fu Q, Gu X, Priest BT, Thomas-Fowlkes B, Weinglass A, Margulis M, Liu J, Pai LY, Hampton C, Haimbach RE, Owens K, Tong V, Xu S, Hu M, Zingaro GJ, Morissette P, Ehrhart J, Roy S, Sullivan K, Pasternak A. Dong S, et al. Among authors: roy s. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2559-2566. doi: 10.1016/j.bmcl.2017.03.086. Epub 2017 Mar 30. Bioorg Med Chem Lett. 2017. PMID: 28431879
Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.
Shen HC, Ding FX, Wang S, Deng Q, Zhang X, Chen Y, Zhou G, Xu S, Chen HS, Tong X, Tong V, Mitra K, Kumar S, Tsai C, Stevenson AS, Pai LY, Alonso-Galicia M, Chen X, Soisson SM, Roy S, Zhang B, Tata JR, Berger JP, Colletti SL. Shen HC, et al. Among authors: roy s. J Med Chem. 2009 Aug 27;52(16):5009-12. doi: 10.1021/jm900725r. J Med Chem. 2009. PMID: 19645482
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