Literature DB >> 21126876

Facile synthesis and biological evaluation of 3,3-diphenylpropanoyl piperazines as T-type calcium channel blockers.

Yeon-hee Choi1, Du Jong Baek, Seon Hee Seo, Jae Kyun Lee, Ae Nim Pae, Yong Seo Cho, Sun-Joon Min.   

Abstract

We have developed a facile synthesis of 3,3-diphenylpropanamides using Meldrum's acid derivatives as amide coupling components. The in vitro biological evaluation of the title compounds led to the identification of compound 1h, which has good inhibitory activity against T-type calcium channel (IC(50) = 0.83 μM).
Copyright © 2010 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2010        PMID： 21126876     DOI： 10.1016/j.bmcl.2010.11.033

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


  2 in total

1.  The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.

Authors:  Zixiu Xiang; Analisa D Thompson; John T Brogan; Michael L Schulte; Bruce J Melancon; Debbie Mi; L Michelle Lewis; Bende Zou; Liya Yang; Ryan Morrison; Tammy Santomango; Frank Byers; Katrina Brewer; Jonathan S Aldrich; Haibo Yu; Eric S Dawson; Min Li; Owen McManus; Carrie K Jones; J Scott Daniels; Corey R Hopkins; Ximin Simon Xie; P Jeffrey Conn; C David Weaver; Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2011-12-21       Impact factor: 4.418

2.  Identification of Potent and Selective Diphenylpropanamide RORγ Inhibitors.

Authors:  Jun R Huh; Erika E Englund; Hang Wang; Ruili Huang; Pengxiang Huang; Fraydoon Rastinejad; James Inglese; Christopher P Austin; Ronald L Johnson; Wenwei Huang; Dan R Littman
Journal:  ACS Med Chem Lett       Date:  2013-01-10       Impact factor: 4.345
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.