Literature DB >> 20621730

Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers.

Jie Eun Lee1, Hun Yeong Koh, Seon Hee Seo, Yi Yeon Baek, Hyewhon Rhim, Yong Seo Cho, Hyunah Choo, Ae Nim Pae.   

Abstract

T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives substituted with arylpiperazinylalkylamines. The oxazoles were synthesized in a convenient convergent synthetic method, and biologically evaluated against alpha(1G) (Ca(V)3.1) T-type calcium channel. Among total 41 oxazole compounds synthesized, the most active one was the compound 10-35 with an IC(50) value of 0.65 microM, which is comparable with that of mibefradil. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20621730     DOI： 10.1016/j.bmcl.2010.05.030

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


  4 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.  Synthesis of highly substituted oxazoles through iodine(III)-mediated reactions of ketones with nitriles.

Authors:  Akio Saito; Nao Hyodo; Yuji Hanzawa
Journal:  Molecules       Date:  2012-09-13       Impact factor: 4.411

3.  Design, synthesis and biological evaluation of 3-(2-aminooxazol-5-yl)-2H-chromen-2-one derivatives.

Authors:  Saloni Kakkar; Sanjiv Kumar; Siong Meng Lim; Kalavathy Ramasamy; Vasudevan Mani; Syed Adnan Ali Shah; Balasubramanian Narasimhan
Journal:  Chem Cent J       Date:  2018-12-04       Impact factor: 4.215

4.  Synthesis, Anticonvulsant and Antinociceptive Activity of New Hybrid Compounds: Derivatives of 3-(3-Methylthiophen-2-yl)-pyrrolidine-2,5-dione.

Authors:  Małgorzata Góra; Anna Czopek; Anna Rapacz; Anna Dziubina; Monika Głuch-Lutwin; Barbara Mordyl; Jolanta Obniska
Journal:  Int J Mol Sci       Date:  2020-08-11       Impact factor: 5.923
  4 in total

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