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Items: 1 to 20 of 87

1.

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.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1692-6. doi: 10.1016/j.bmcl.2011.01.089. Epub 2011 Jan 26.

PMID:
21316226
2.

Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.

Jo MN, Seo HJ, Kim Y, Seo SH, Rhim H, Cho YS, Cha JH, Koh HY, Choo H, Pae AN.

Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.

PMID:
17035033
3.

Lead discovery and optimization of T-type calcium channel blockers.

Park JH, Choi JK, Lee E, Lee JK, Rhim H, Seo SH, Kim Y, Doddareddy MR, Pae AN, Kang J, Roh EJ.

Bioorg Med Chem. 2007 Feb 1;15(3):1409-19. Epub 2006 Nov 10.

PMID:
17150365
4.

In vitro characterization of T-type calcium channel antagonist TTA-A2 and in vivo effects on arousal in mice.

Kraus RL, Li Y, Gregan Y, Gotter AL, Uebele VN, Fox SV, Doran SM, Barrow JC, Yang ZQ, Reger TS, Koblan KS, Renger JJ.

J Pharmacol Exp Ther. 2010 Nov;335(2):409-17. doi: 10.1124/jpet.110.171058. Epub 2010 Aug 3.

5.

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.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5147-52. doi: 10.1016/j.bmcl.2010.07.010. Epub 2010 Jul 8.

PMID:
20673719
6.

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.

J Med Chem. 2008 Oct 23;51(20):6471-7. doi: 10.1021/jm800830n. Epub 2008 Sep 26.

PMID:
18817368
7.

Towards the discovery of novel T-type calcium channel blockers.

Lory P, Chemin J.

Expert Opin Ther Targets. 2007 May;11(5):717-22. Review.

PMID:
17465728
8.

Design, synthesis, and biological evaluation of 1,3-dioxoisoindoline-5-carboxamide derivatives as T-type calcium channel blockers.

Kim HS, Kim Y, Doddareddy MR, Seo SH, Rhim H, Tae J, Pae AN, Choo H, Cho YS.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):476-81. Epub 2006 Oct 21.

PMID:
17092715
9.

Synthesis and SAR studies of a novel series of T-type calcium channel blockers.

Park SJ, Park SJ, Lee MJ, Rhim H, Kim Y, Lee JH, Chung BY, Lee JY.

Bioorg Med Chem. 2006 May 15;14(10):3502-11. Epub 2006 Jan 24.

PMID:
16434203
10.

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.

J Med Chem. 2008 Jul 10;51(13):3692-5. doi: 10.1021/jm800419w. Epub 2008 Jun 10.

PMID:
18540666
11.

Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.

Hangeland JJ, Cheney DL, Friends TJ, Swartz S, Levesque PC, Rich AJ, Sun L, Bridal TR, Adam LP, Normandin DE, Murugesan N, Ewing WR.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):474-8. Epub 2007 Dec 3.

PMID:
18160281
12.

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.

Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7.

PMID:
19582593
13.

Novel potent and selective calcium-release-activated calcium (CRAC) channel inhibitors. Part 1: synthesis and inhibitory activity of 5-(1-methyl-3-trifluoromethyl-1H-pyrazol-5-yl)-2-thiophenecarboxamides.

Yonetoku Y, Kubota H, Okamoto Y, Toyoshima A, Funatsu M, Ishikawa J, Takeuchi M, Ohta M, Tsukamoto S.

Bioorg Med Chem. 2006 Jul 15;14(14):4750-60. Epub 2006 Mar 31.

PMID:
16580212
14.

Scaffold-based design and synthesis of potent N-type calcium channel blockers.

Zamponi GW, Feng ZP, Zhang L, Pajouhesh H, Ding Y, Belardetti F, Pajouhesh H, Dolphin D, Mitscher LA, Snutch TP.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72. doi: 10.1016/j.bmcl.2009.09.008. Epub 2009 Sep 11.

PMID:
19815411
15.

3D pharmacophore based virtual screening of T-type calcium channel blockers.

Doddareddy MR, Choo H, Cho YS, Rhim H, Koh HY, Lee JH, Jeong SW, Pae AN.

Bioorg Med Chem. 2007 Jan 15;15(2):1091-105. Epub 2006 Oct 30.

PMID:
17074493
16.

Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers.

Rhim H, Lee YS, Park SJ, Chung BY, Lee JY.

Bioorg Med Chem Lett. 2005 Jan 17;15(2):283-6.

PMID:
15603940
17.

Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers.

Ku IW, Cho S, Doddareddy MR, Jang MS, Keum G, Lee JH, Chung BY, Kim Y, Rhim H, Kang SB.

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5244-8. Epub 2006 Jul 28.

PMID:
16876404
18.

T-type calcium channels inhibitors: a patent review.

Giordanetto F, Knerr L, Wållberg A.

Expert Opin Ther Pat. 2011 Jan;21(1):85-101. doi: 10.1517/13543776.2011.536532. Epub 2010 Nov 19. Review.

PMID:
21087200
19.

Effect of T-type selective calcium antagonist on renal microcirculation: studies in the isolated perfused hydronephrotic kidney.

Ozawa Y, Hayashi K, Nagahama T, Fujiwara K, Saruta T.

Hypertension. 2001 Sep;38(3):343-7.

20.

Synthesis and biological evaluation of novel T-type calcium channel blockers.

Choi JY, Seo HN, Lee MJ, Park SJ, Park SJ, Jeon JY, Kang JH, Pae AN, Rhim H, Lee JY.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):471-5. Epub 2006 Oct 12.

PMID:
17064894
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