Literature DB >> 15603940

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

Hyewhon Rhim1, Yong Sup Lee, Seong Jun Park, Bong Young Chung, Jae Yeol Lee.   

Abstract

We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca(2+) channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca(2+) channels and N-type Ca(2+) channels. Among them, 5b (KYS05044, IC(50)=0.56+/-0.10 microM) was identified as potent T-type Ca(2+) channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI=>100).

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 15603940     DOI: 10.1016/j.bmcl.2004.10.078

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


  4 in total

1.  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

2.  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

3.  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

4.  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

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.