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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: hernandez m. 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: hernandez m. 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: hernandez m. 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: hernandez m. 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: hernandez m. 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: hernandez m. 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
Heterozygous disruption of renal outer medullary potassium channel in rats is associated with reduced blood pressure.
Zhou X, Zhang Z, Shin MK, Horwitz SB, Levorse JM, Zhu L, Sharif-Rodriguez W, Streltsov DY, Dajee M, Hernandez M, Pan Y, Urosevic-Price O, Wang L, Forrest G, Szeto D, Zhu Y, Cui Y, Michael B, Balogh LA, Welling PA, Wade JB, Roy S, Sullivan KA. Zhou X, et al. Among authors: hernandez m. Hypertension. 2013 Aug;62(2):288-94. doi: 10.1161/HYPERTENSIONAHA.111.01051. Epub 2013 Jun 10. Hypertension. 2013. PMID: 23753405
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
Singh SB, Ondeyka JG, Liu W, Chen S, Chen TS, Li X, Bouffard A, Dropinski J, Jones AB, McCormick S, Hayes N, Wang J, Sharma N, Macnaul K, Hernandez M, Chao YS, Baffic J, Lam MH, Burton C, Sparrow CP, Menke JG. Singh SB, et al. Among authors: hernandez m. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2824-8. doi: 10.1016/j.bmcl.2005.03.100. Bioorg Med Chem Lett. 2005. PMID: 15911262
4,632 results