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Page 1
Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1).
Ye XY, Chen SY, Nayeem A, Golla R, Seethala R, Wang M, Harper T, Sleczka BG, Li YX, He B, Kirby M, Gordon DA, Robl JA. Ye XY, et al. Among authors: harper t. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6699-704. doi: 10.1016/j.bmcl.2011.09.055. Epub 2011 Sep 21. Bioorg Med Chem Lett. 2011. PMID: 21983439
Synthesis and structure-activity relationship of 2-adamantylmethyl tetrazoles as potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
Ye XY, Yoon D, Chen SY, Nayeem A, Golla R, Seethala R, Wang M, Harper T, Sleczka BG, Apedo A, Li YX, He B, Kirby M, Gordon DA, Robl JA. Ye XY, et al. Among authors: harper t. Bioorg Med Chem Lett. 2014 Jan 15;24(2):654-60. doi: 10.1016/j.bmcl.2013.11.066. Epub 2013 Dec 5. Bioorg Med Chem Lett. 2014. PMID: 24360604
Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).
Li J, Kennedy LJ, Wang H, Li JJ, Walker SJ, Hong Z, O'Connor SP, Nayeem A, Camac DM, Morin PE, Sheriff S, Wang M, Harper T, Golla R, Seethala R, Harrity T, Ponticiello RP, Morgan NN, Taylor JR, Zebo R, Gordon DA, Robl JA. Li J, et al. Among authors: harper t. ACS Med Chem Lett. 2014 May 22;5(7):803-8. doi: 10.1021/ml500144h. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050169 Free PMC article.
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists.
Carpenter J, Wang Y, Wu G, Feng J, Ye XY, Morales CL, Broekema M, Rossi KA, Miller KJ, Murphy BJ, Wu G, Malmstrom SE, Azzara AV, Sher PM, Fevig JM, Alt A, Bertekap RL Jr, Cullen MJ, Harper TM, Foster K, Luk E, Xiang Q, Grubb MF, Robl JA, Wacker DA. Carpenter J, et al. J Med Chem. 2017 Jul 27;60(14):6166-6190. doi: 10.1021/acs.jmedchem.7b00385. Epub 2017 Jul 7. J Med Chem. 2017. PMID: 28635286
Neutral macrocyclic factor VIIa inhibitors.
Wurtz NR, Parkhurst BL, DeLucca I, Glunz PW, Jiang W, Zhang X, Cheney DL, Bozarth JM, Rendina AR, Wei A, Harper T, Luettgen JM, Wu Y, Wong PC, Seiffert DA, Wexler RR, Priestley ES. Wurtz NR, et al. Among authors: harper t. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2650-2654. doi: 10.1016/j.bmcl.2017.04.008. Epub 2017 Apr 19. Bioorg Med Chem Lett. 2017. PMID: 28460818
Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists.
Finlay HJ, Jiang J, Caringal Y, Kover A, Conder ML, Xing D, Levesque P, Harper T, Hsueh MM, Atwal K, Blanar M, Wexler R, Lloyd J. Finlay HJ, et al. Among authors: harper t. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1743-7. doi: 10.1016/j.bmcl.2013.01.064. Epub 2013 Jan 26. Bioorg Med Chem Lett. 2013. PMID: 23414837
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Clark CG, Rossi KA, Corte JR, Fang T, Smallheer JM, De Lucca I, Nirschl DS, Orwat MJ, Pinto DJP, Hu Z, Wang Y, Yang W, Jeon Y, Ewing WR, Myers JE Jr, Sheriff S, Lou Z, Bozarth JM, Wu Y, Rendina A, Harper T, Zheng J, Xin B, Xiang Q, Luettgen JM, Seiffert DA, Wexler RR, Lam PYS. Clark CG, et al. Among authors: harper t. Bioorg Med Chem Lett. 2019 Oct 1;29(19):126604. doi: 10.1016/j.bmcl.2019.08.008. Epub 2019 Aug 16. Bioorg Med Chem Lett. 2019. PMID: 31445854
Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.
Zhang X, Jiang W, Jacutin-Porte S, Glunz PW, Zou Y, Cheng X, Nirschl AH, Wurtz NR, Luettgen JM, Rendina AR, Luo G, Harper TM, Wei A, Anumula R, Cheney DL, Knabb RM, Wong PC, Wexler RR, Priestley ES. Zhang X, et al. ACS Med Chem Lett. 2013 Dec 26;5(2):188-92. doi: 10.1021/ml400453z. eCollection 2014 Feb 13. ACS Med Chem Lett. 2013. PMID: 24900796 Free PMC article.
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.
Zhang X, Glunz PW, Johnson JA, Jiang W, Jacutin-Porte S, Ladziata V, Zou Y, Phillips MS, Wurtz NR, Parkhurst B, Rendina AR, Harper TM, Cheney DL, Luettgen JM, Wong PC, Seiffert D, Wexler RR, Priestley ES. Zhang X, et al. J Med Chem. 2016 Aug 11;59(15):7125-37. doi: 10.1021/acs.jmedchem.6b00469. Epub 2016 Aug 2. J Med Chem. 2016. PMID: 27455395
277 results