Literature DB >> 17064894

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

Ja Youn Choi1, Han Na Seo, Min Joo Lee, Seong Jun Park, Sung Jun Park, Ji Young Jeon, Joo Hi Kang, Ae Nim Pae, Hyewhon Rhim, Jae Yeol Lee.   

Abstract

3,4-Dihydroquinazoline analogues substituted by N-methyl-N-(5-pyrrolidinopentyl)amine at the 2-position were synthesized and their blocking effects were evaluated for T- and N-type calcium channels. Compound 11b (KYS05080), compared to mibefradil (IC50=1.34+/-0.49 microM), was about 5-fold potent (IC50=0.26+/-0.01 microM) for T-type calcium channel (alpha1G) blocking and its selectivity of T/N-type was also improved (7.5 versus 1.4 of mibefradil).

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Year:  2006        PMID： 17064894     DOI： 10.1016/j.bmcl.2006.10.024

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


  6 in total

1.  Redox-active magnetic resonance imaging contrast agents: studies with thiol-bearing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetracetic acid derivatives.

Authors:  Bhumasamudram Jagadish; Gerald P Guntle; Dezheng Zhao; Vijay Gokhale; Tarik J Ozumerzifon; Ali M Ahad; Eugene A Mash; Natarajan Raghunand
Journal:  J Med Chem       Date:  2012-11-28       Impact factor: 7.446

Review 2.  T-type Ca2+ channels and the urinary and male genital tracts.

Authors:  C H Fry; R I Jabr
Journal:  Pflugers Arch       Date:  2014-01-25       Impact factor: 3.657

3.  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

4.  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

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.  Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.

Authors:  Anqi Ma; Wenyu Yu; Fengling Li; Rachel M Bleich; J Martin Herold; Kyle V Butler; Jacqueline L Norris; Victoria Korboukh; Ashutosh Tripathy; William P Janzen; Cheryl H Arrowsmith; Stephen V Frye; Masoud Vedadi; Peter J Brown; Jian Jin
Journal:  J Med Chem       Date:  2014-07-25       Impact factor: 7.446
  6 in total

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