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Items: 1 to 20 of 106

1.

Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain.

Beebe X, Yeung CM, Darczak D, Shekhar S, Vortherms TA, Miller L, Milicic I, Swensen AM, Zhu CZ, Banfor P, Wetter JM, Marsh KC, Jarvis MF, Scott VE, Schrimpf MR, Lee CH.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4857-61. doi: 10.1016/j.bmcl.2013.06.074.

PMID:
23876987
2.

Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers.

Seko T, Kato M, Kohno H, Ono S, Hashimura K, Takimizu H, Nakai K, Maegawa H, Katsube N, Toda M.

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2067-70.

PMID:
11514140
3.

Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca²⁺ channel blockers with analgesic activity.

Beebe X, Darczak D, Henry RF, Vortherms T, Janis R, Namovic M, Donnelly-Roberts D, Kage KL, Surowy C, Milicic I, Niforatos W, Swensen A, Marsh KC, Wetter JM, Franklin P, Baker S, Zhong C, Simler G, Gomez E, Boyce-Rustay JM, Zhu CZ, Stewart AO, Jarvis MF, Scott VE.

Bioorg Med Chem. 2012 Jul 1;20(13):4128-39. doi: 10.1016/j.bmc.2012.04.057.

PMID:
22626552
4.

Discovery and SAR of a novel series of 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles as N-type calcium channel inhibitors.

Winters MP, Subasinghe N, Wall M, Beck E, Brandt MR, Finley MF, Liu Y, Lubin ML, Neeper MP, Qin N, Flores CM, Sui Z.

Bioorg Med Chem Lett. 2014 May 1;24(9):2057-61. doi: 10.1016/j.bmcl.2014.03.063.

PMID:
24726803
5.

A novel series of pyrazolylpiperidine N-type calcium channel blockers.

Subasinghe NL, Wall MJ, Winters MP, Qin N, Lubin ML, Finley MF, Brandt MR, Neeper MP, Schneider CR, Colburn RW, Flores CM, Sui Z.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4080-3. doi: 10.1016/j.bmcl.2012.04.075.

PMID:
22608964
6.

Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.

Pajouhesh H, Feng ZP, Ding Y, Zhang L, Pajouhesh H, Morrison JL, Belardetti F, Tringham E, Simonson E, Vanderah TW, Porreca F, Zamponi GW, Mitscher LA, Snutch TP.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1378-83. doi: 10.1016/j.bmcl.2010.01.008.

PMID:
20117000
7.

Discovery and evaluation of selective N-type calcium channel blockers: 6-unsubstituted-1,4-dihydropyridine-5-carboxylic acid derivatives.

Yamamoto T, Niwa S, Tokumasu M, Onishi T, Ohno S, Hagihara M, Koganei H, Fujita S, Takeda T, Saitou Y, Iwayama S, Takahara A, Iwata S, Shoji M.

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3639-42. doi: 10.1016/j.bmcl.2012.04.051.

PMID:
22560585
8.

Discovery of novel tetrahydroisoquinoline derivatives as orally active N-type calcium channel blockers with high selectivity for hERG potassium channels.

Ogiyama T, Inoue M, Honda S, Yamada H, Watanabe T, Gotoh T, Kiso T, Koakutsu A, Kakimoto S, Shishikura J.

Bioorg Med Chem. 2014 Dec 15;22(24):6899-907. doi: 10.1016/j.bmc.2014.10.020. Erratum in: Bioorg Med Chem. 2015 Sep 1;23(17):6079.

PMID:
25456079
9.

Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain.

Myatt JW, Healy MP, Bravi GS, Billinton A, Johnson CN, Matthews KL, Jandu KS, Meng W, Hersey A, Livermore DG, Douault CB, Witherington J, Bit RA, Rowedder JE, Brown JD, Clayton NM.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4683-8. doi: 10.1016/j.bmcl.2010.05.026.

PMID:
20566291
10.

Discovery and SAR of novel tetrahydropyrrolo[3,4-c]pyrazoles as inhibitors of the N-type calcium channel.

Winters MP, Subasinghe N, Wall M, Beck E, Brandt MR, Finley MF, Liu Y, Lubin ML, Neeper MP, Qin N, Flores CM, Sui Z.

Bioorg Med Chem Lett. 2014 May 1;24(9):2053-6. doi: 10.1016/j.bmcl.2014.03.062.

PMID:
24726802
11.

Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain.

Teodori E, Baldi E, Dei S, Gualtieri F, Romanelli MN, Scapecchi S, Bellucci C, Ghelardini C, Matucci R.

J Med Chem. 2004 Nov 18;47(24):6070-81.

PMID:
15537361
12.

Structure-activity relationships of trimethoxybenzyl piperazine N-type calcium channel inhibitors.

Pajouhesh H, Feng ZP, Zhang L, Pajouhesh H, Jiang X, Hendricson A, Dong H, Tringham E, Ding Y, Vanderah TW, Porreca F, Belardetti F, Zamponi GW, Mitscher LA, Snutch TP.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4153-8. doi: 10.1016/j.bmcl.2012.04.054.

13.

The discovery of [1-(4-dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethylbutyl)-phen yl]-(3-methyl-but-2-enyl)-amine, an N-type Ca+2 channel blocker with oral activity for analgesia.

Hu LY, Ryder TR, Rafferty MF, Taylor CP, Feng MR, Kuo BS, Lotarski SM, Miljanich GP, Millerman E, Siebers KM, Szoke BG.

Bioorg Med Chem. 2000 Jun;8(6):1203-12.

PMID:
10896101
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.

PMID:
19815411
15.

L-Cysteine based N-type calcium channel blockers: structure-activity relationships of the C-terminal lipophilic moiety, and oral analgesic efficacy in rat pain models.

Seko T, Kato M, Kohno H, Ono S, Hashimura K, Takenobu Y, Takimizu H, Nakai K, Maegawa H, Katsube N, Toda M.

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2267-9.

PMID:
12161113
16.

Discovery of diphenyl lactam derivatives as N-type calcium channel blockers.

Doherty GA, Bhatia P, Vortherms TA, Marsh KC, Wetter JM, Mack H, Scott VE, Jarvis MF, Stewart AO.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1716-8. doi: 10.1016/j.bmcl.2011.12.100.

PMID:
22277280
17.
18.

Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers.

Knutsen LJ, Hobbs CJ, Earnshaw CG, Fiumana A, Gilbert J, Mellor SL, Radford F, Smith NJ, Birch PJ, Russell Burley J, Ward SD, James IF.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):662-7.

PMID:
17134896
19.

The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels.

Yamamoto T, Niwa S, Ohno S, Tokumasu M, Masuzawa Y, Nakanishi C, Nakajo A, Onishi T, Koganei H, Fujita S, Takeda T, Kito M, Ono Y, Saitou Y, Takahara A, Iwata S, Shoji M.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4813-6. doi: 10.1016/j.bmcl.2008.07.096.

PMID:
18684623
20.

3-Benzamides and 3,4,5-trimethoxyphenyl amines as calcium channel blockers.

Kang B, Oh JA, Lee JY, Rhim H, Yune TY, Park Choo HY.

Bioorg Med Chem. 2015 Sep 15;23(18):6166-72. doi: 10.1016/j.bmc.2015.07.067.

PMID:
26296911
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