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Page 1
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
Shipe WD, Barrow JC, Yang ZQ, Lindsley CW, Yang FV, Schlegel KA, Shu Y, Rittle KE, Bock MG, Hartman GD, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Uebele VN, Nuss CE, Connolly TM, Doran SM, Fox SV, Kraus RL, Marino MJ, Graufelds VK, Vargas HM, Bunting PB, Hasbun-Manning M, Evans RM, Koblan KS, Renger JJ. Shipe WD, et al. Among authors: ballard je. J Med Chem. 2008 Jul 10;51(13):3692-5. doi: 10.1021/jm800419w. Epub 2008 Jun 10. J Med Chem. 2008. PMID: 18540666
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Yang ZQ, Barrow JC, Shipe WD, Schlegel KA, Shu Y, Yang FV, Lindsley CW, Rittle KE, Bock MG, Hartman GD, Uebele VN, Nuss CE, Fox SV, Kraus RL, Doran SM, Connolly TM, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Marino MJ, Graufelds VK, DiLella AG, Reynolds IJ, Vargas HM, Bunting PB, Woltmann RF, Magee MM, Koblan KS, Renger JJ. Yang ZQ, et al. Among authors: ballard je. J Med Chem. 2008 Oct 23;51(20):6471-7. doi: 10.1021/jm800830n. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817368
Antagonism of T-type calcium channels inhibits high-fat diet-induced weight gain in mice.
Uebele VN, Gotter AL, Nuss CE, Kraus RL, Doran SM, Garson SL, Reiss DR, Li Y, Barrow JC, Reger TS, Yang ZQ, Ballard JE, Tang C, Metzger JM, Wang SP, Koblan KS, Renger JJ. Uebele VN, et al. Among authors: ballard je. J Clin Invest. 2009 Jun;119(6):1659-67. doi: 10.1172/JCI36954. Epub 2009 May 18. J Clin Invest. 2009. PMID: 19451696 Free PMC article.
Positive allosteric interaction of structurally diverse T-type calcium channel antagonists.
Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ. Uebele VN, et al. Among authors: ballard je. Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7. Cell Biochem Biophys. 2009. PMID: 19582593
Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists.
Schlegel KA, Yang ZQ, Reger TS, Shu Y, Cube R, Rittle KE, Bondiskey P, Bock MG, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Kraus RL, Li Y, Uebele VN, Renger JJ, Barrow JC. Schlegel KA, et al. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5147-52. doi: 10.1016/j.bmcl.2010.07.010. Epub 2010 Jul 8. Bioorg Med Chem Lett. 2010. PMID: 20673719
Pyridyl amides as potent inhibitors of T-type calcium channels.
Reger TS, Yang ZQ, Schlegel KA, Shu Y, Mattern C, Cube R, Rittle KE, McGaughey GB, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Renger JJ, Barrow JC. Reger TS, et al. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1692-6. doi: 10.1016/j.bmcl.2011.01.089. Epub 2011 Jan 26. Bioorg Med Chem Lett. 2011. PMID: 21316226
Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists.
Barrow JC, Rittle KE, Reger TS, Yang ZQ, Bondiskey P, McGaughey GB, Bock MG, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Kraus RL, Li Y, Marino MJ, Kuzmick Graufelds V, Uebele VN, Renger JJ. Barrow JC, et al. ACS Med Chem Lett. 2010 Feb 1;1(2):75-9. doi: 10.1021/ml100004r. eCollection 2010 May 13. ACS Med Chem Lett. 2010. PMID: 24900180 Free PMC article.
Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.
Yang ZQ, Schlegel KA, Shu Y, Reger TS, Cube R, Mattern C, Coleman PJ, Small J, Hartman GD, Ballard J, Tang C, Kuo Y, Prueksaritanont T, Nuss CE, Doran S, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Taylor AB, Zeng W, Fang W, Chavez-Eng C, Troyer MD, Luk JA, Laethem T, Cook WO, Renger JJ, Barrow JC. Yang ZQ, et al. ACS Med Chem Lett. 2010 Aug 24;1(9):504-9. doi: 10.1021/ml100170e. eCollection 2010 Dec 9. ACS Med Chem Lett. 2010. PMID: 24900239 Free PMC article.
53 results