Literature DB >> 16434203

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

Seong Jun Park1, Sung Jun Park, Min Joo Lee, Hyewhon Rhim, Yoonjee Kim, Jung-Ha Lee, Bong Young Chung, Jae Yeol Lee.   

Abstract

For the novel, potent, and selective T-type Ca2+ channel blockers, a series of sulfonamido-containing 3,4-dihydroquinazoline derivatives were prepared and evaluated for their blocking actions on T- and N-type Ca2+ channels. Among them, 9c (KYS05064, IC50 = 0.96 +/- 0.22 microM) was found to be as potent as Mibefradil and also showed the highest selectivity for T-type Ca2+ channel with no effect on N-type Ca2+ channel.

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Year:  2006        PMID: 16434203     DOI: 10.1016/j.bmc.2006.01.005

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  6 in total

Review 1.  Low-voltage-activated T-type Ca2+ channel inhibitors as new tools in the treatment of glioblastoma: the role of endostatin.

Authors:  Yuan Zhang; Hua Wang; Zhiyuan Qian; Bo Feng; Xianyang Zhao; Xinghong Jiang; Jin Tao
Journal:  Pflugers Arch       Date:  2014-01-10       Impact factor: 3.657

2.  T-type calcium channel antagonists suppress tremor in two mouse models of essential tremor.

Authors:  Adrian Handforth; Gregg E Homanics; Douglas F Covey; Kathiresan Krishnan; Jae Yeol Lee; Kenji Sakimura; Fredricka C Martin; Arnulfo Quesada
Journal:  Neuropharmacology       Date:  2010-06-12       Impact factor: 5.250

Review 3.  T-type calcium channel as a new therapeutic target for tremor.

Authors:  Hideto Miwa; Tomoyoshi Kondo
Journal:  Cerebellum       Date:  2011-09       Impact factor: 3.847

4.  Ionic liquid-supported synthesis of dihydroquinazolines and tetrahydroquinazolines under microwave irradiation.

Authors:  Hai-Yuan Hsu; Chih-Chun Tseng; Banrali Matii; Chung-Ming Sun
Journal:  Mol Divers       Date:  2011-12-17       Impact factor: 2.943

5.  In silico identification of T-type calcium channel blockers: A ligand-based pharmacophore mapping approach.

Authors:  Tamanna Gandhi; Anu R Melge; C Gopi Mohan
Journal:  J Adv Res       Date:  2016-09-16       Impact factor: 10.479

6.  Synthesis of dihydroquinazolines from 2-aminobenzylamine: N 3 -aryl derivatives with electron-withdrawing groups.

Authors:  Nadia Gruber; Jimena E Díaz; Liliana R Orelli
Journal:  Beilstein J Org Chem       Date:  2018-09-26       Impact factor: 2.883

  6 in total

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