Literature DB >> 15177437

3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers.

Yong Sup Lee1, Bum Hoon Lee, Seong Jun Park, Soon Bang Kang, Hyewhon Rhim, Jin-Yong Park, Jung-Ha Lee, Seong-Woo Jeong, Jae Yeol Lee.   

Abstract

For LVA T-type Ca2+ channel blockers, 3,4-dihydroquinazoline derivatives as new scaffolds were prepared and evaluated for the inhibitory activity against two members of the recombinant T-type Ca2+ channel family. Among them, 8a (KYS05001, IC50=0.9 microM) was nearly equipotent with mibefradil (IC50=0.84 microM) and inhibited LVA T-type Ca2+ channel with greater efficacy than HVA Ca2+ channel.

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Year:  2004        PMID： 15177437     DOI： 10.1016/j.bmcl.2004.04.090

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 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.  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

3.  Friedel-Crafts synthesis of bis(trifluoromethylated)-4-aryl-3,4-dihydroquinazolines, bis(trifluoromethylated)-3,4-dihydroquinazoline-4-ols and trifluoromethyl arylketoimines using N-aryltrifluoroacetimidoyl chlorides and benzene derivatives.

Authors:  Elham Kazemi; Ali Darehkordi; Alireza Abbasi
Journal:  Mol Divers       Date:  2021-02-03       Impact factor: 2.943

4.  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

5.  Syntheses of 3,4- and 1,4-dihydroquinazolines from 2-aminobenzylamine.

Authors:  Jimena E Díaz; Silvia Ranieri; Nadia Gruber; Liliana R Orelli
Journal:  Beilstein J Org Chem       Date:  2017-07-27       Impact factor: 2.883

6.  A bifunctional iminophosphorane squaramide catalyzed enantioselective synthesis of hydroquinazolines via intramolecular aza-Michael reaction to α,β-unsaturated esters.

Authors:  Guanglong Su; Connor J Thomson; Ken Yamazaki; Daniel Rozsar; Kirsten E Christensen; Trevor A Hamlin; Darren J Dixon
Journal:  Chem Sci       Date:  2021-03-18       Impact factor: 9.825

7.  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
  7 in total

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