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Page 1
Evaluation of selective inhibitors of 11β-HSD1 for the treatment of hypertension.
Bauman DR, Whitehead A, Contino LC, Cui J, Garcia-Calvo M, Gu X, Kevin N, Ma X, Pai LY, Shah K, Shen X, Stribling S, Zokian HJ, Metzger J, Shevell DE, Waddell ST. Bauman DR, et al. Among authors: pai ly. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3650-3. doi: 10.1016/j.bmcl.2013.03.011. Epub 2013 Mar 22. Bioorg Med Chem Lett. 2013. PMID: 23659858
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Hoyt SB, Park MK, London C, Xiong Y, Tata J, Bennett DJ, Cooke A, Cai J, Carswell E, Robinson J, MacLean J, Brown L, Belshaw S, Clarkson TR, Liu K, Liang GB, Struthers M, Cully D, Wisniewski T, Ren N, Bopp C, Sok A, Cai TQ, Stribling S, Pai LY, Ma X, Metzger J, Verras A, McMasters D, Chen Q, Tung E, Tang W, Salituro G, Buist N, Kuethe J, Rivera N, Clemas J, Zhou G, Gibson J, Maxwell CA, Lassman M, McLaughlin T, Castro-Perez J, Szeto D, Forrest G, Hajdu R, Rosenbach M, Ali A. Hoyt SB, et al. Among authors: pai ly. ACS Med Chem Lett. 2015 Apr 7;6(5):573-8. doi: 10.1021/acsmedchemlett.5b00054. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005536 Free PMC article.
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Hoyt SB, Petrilli W, London C, Liang GB, Tata J, Hu Q, Yin L, van Koppen CJ, Hartmann RW, Struthers M, Wisniewski T, Ren N, Bopp C, Sok A, Cai TQ, Stribling S, Pai LY, Ma X, Metzger J, Verras A, McMasters D, Chen Q, Tung E, Tang W, Salituro G, Buist N, Clemas J, Zhou G, Gibson J, Maxwell CA, Lassman M, McLaughlin T, Castro-Perez J, Szeto D, Forrest G, Hajdu R, Rosenbach M, Xiong Y. Hoyt SB, et al. Among authors: pai ly. ACS Med Chem Lett. 2015 Jul 17;6(8):861-5. doi: 10.1021/acsmedchemlett.5b00048. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288685 Free PMC article.
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: pai ly. 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 spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.
Shen HC, Ding FX, Wang S, Xu S, Chen HS, Tong X, Tong V, Mitra K, Kumar S, Zhang X, Chen Y, Zhou G, Pai LY, Alonso-Galicia M, Chen X, Zhang B, Tata JR, Berger JP, Colletti SL. Shen HC, et al. Among authors: pai ly. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3398-404. doi: 10.1016/j.bmcl.2009.05.036. Epub 2009 May 18. Bioorg Med Chem Lett. 2009. PMID: 19481932
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: pai ly. 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
The design and synthesis of novel spirocyclic heterocyclic sulfone ROMK inhibitors as diuretics.
Chobanian HR, Guo Y, Pio B, Tang H, Teumelsan N, Clements M, Frie J, Ferguson R, Guo Z, Thomas-Fowlkes BS, Felix JP, Liu J, Kohler M, Priest B, Hampton C, Pai LY, Corona A, Metzger J, Tong V, Joshi EM, Xu L, Owens K, Maloney K, Sullivan K, Pasternak A. Chobanian HR, et al. Among authors: pai ly. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1109-1114. doi: 10.1016/j.bmcl.2016.10.032. Epub 2016 Oct 13. Bioorg Med Chem Lett. 2017. PMID: 28111141
Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic.
Jiang J, Ding FX, Zhou X, Bateman TJ, Dong S, Gu X, Keh deJesus R, Pio B, Tang H, Chobanian HR, Levorse D, Hu M, Thomas-Fowlkes B, Margulis M, Koehler M, Weinglass A, Gibson J, Houle K, Yudkovitz J, Hampton C, Pai LY, Samuel K, Cutarelli T, Sullivan K, Parmee ER, Davies I, Pasternak A. Jiang J, et al. Among authors: pai ly. J Med Chem. 2021 Jun 10;64(11):7691-7701. doi: 10.1021/acs.jmedchem.1c00406. Epub 2021 May 26. J Med Chem. 2021. PMID: 34038119
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.
Shen HC, Ding FX, Deng Q, Xu S, Chen HS, Tong X, Tong V, Zhang X, Chen Y, Zhou G, Pai LY, Alonso-Galicia M, Zhang B, Roy S, Tata JR, Berger JP, Colletti SL. Shen HC, et al. Among authors: pai ly. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5314-20. doi: 10.1016/j.bmcl.2009.07.138. Epub 2009 Aug 6. Bioorg Med Chem Lett. 2009. PMID: 19682899
Soluble guanylate cyclase stimulators for the treatment of hypertension: Discovery of MK-2947.
Brockunier L, Stelmach J, Guo J, Spencer T, Rosauer K, Bansal A, Cai SJ, Chen N, Cummings J, Huang L, Johnson T, Levesque S, Luo L, Maloney K, Metzger J, Mortko C, Ortega K, Pai LY, Pereira A, Salituro G, Shang J, Shepherd C, Sherrie Xu S, Yang Q, Cui J, Roy S, Parmee E, Raghavan S. Brockunier L, et al. Among authors: pai ly. Bioorg Med Chem Lett. 2020 Nov 1;30(21):127574. doi: 10.1016/j.bmcl.2020.127574. Epub 2020 Sep 24. Bioorg Med Chem Lett. 2020. PMID: 32980512
34 results