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Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain.
Chobanian HR, Guo Y, Liu P, Chioda MD, Fung S, Lanza TJ, Chang L, Bakshi RK, Dellureficio JP, Hong Q, McLaughlin M, Belyk KM, Krska SW, Makarewicz AK, Martel EJ, Leone JF, Frey L, Karanam B, Madeira M, Alvaro R, Shuman J, Salituro G, Terebetski JL, Jochnowitz N, Mistry S, McGowan E, Hajdu R, Rosenbach M, Abbadie C, Alexander JP, Shiao LL, Sullivan KM, Nargund RP, Wyvratt MJ, Lin LS, DeVita RJ. Chobanian HR, et al. Among authors: sullivan km. ACS Med Chem Lett. 2014 Apr 10;5(6):717-21. doi: 10.1021/ml5001239. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944750 Free PMC article.
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. 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
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. 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 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. 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.
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. 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
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. 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
631 results