Literature DB >> 15246072

Synthesis and biological evaluation of novel T-type Ca2+ channel blockers.

Hee Kyung Jung1, Munikumar Reddy Doddareddy, Joo Hwan Cha, Hyewhon Rhim, Yong Seo Cho, Hun Yeong Koh, Bong Young Jung, Ae Nim Pae.   

Abstract

A small molecule library of piperazinylalkylisoxazole derivatives containing about 600 compounds was designed, synthesized and evaluated for blocking effects on T-type Ca(2+) channel. Several ligands were identified to possess high inhibitory activity against the T-type Ca(2+) channel. The compound 21 with trifluoromethyl substituents at C(3)-position of phenyl group (R(1)) and C(2)-position of phenyl group (R(2)) showed the highest inhibitory activity with IC(50) value of 1.02 microM, which is comparable to that of mibefradil.

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Year:  2004        PMID: 15246072     DOI: 10.1016/j.bmc.2004.06.011

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  5 in total

1.  Design, synthesis, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors.

Authors:  Enza Lacivita; Paola De Giorgio; Irene T Lee; Sean I Rodeheaver; Bryan A Weiss; Claudia Fracasso; Silvio Caccia; Francesco Berardi; Roberto Perrone; Ming-Rong Zhang; Jun Maeda; Makoto Higuchi; Tetsuya Suhara; John A Schetz; Marcello Leopoldo
Journal:  J Med Chem       Date:  2010-10-28       Impact factor: 7.446

2.  Synthesis, Antiinflammatory and Antibacterial Activity of Novel Indolyl-isoxazoles.

Authors:  S S Panda; P V R Chowdary; B S Jayashree
Journal:  Indian J Pharm Sci       Date:  2009-11       Impact factor: 0.975

3.  Isoxazole derivatives as new nitric oxide elicitors in plants.

Authors:  Anca Oancea; Emilian Georgescu; Florentina Georgescu; Alina Nicolescu; Elena Iulia Oprita; Catalina Tudora; Lucian Vladulescu; Marius-Constantin Vladulescu; Florin Oancea; Calin Deleanu
Journal:  Beilstein J Org Chem       Date:  2017-04-06       Impact factor: 2.883

4.  Synthesis, Antimicrobial and Antioxidant Activities of 2-Isoxazoline Derivatives.

Authors:  Asma Alshamari; Mahmoud Al-Qudah; Fedaa Hamadeh; Lo'ay Al-Momani; Sultan Abu-Orabi
Journal:  Molecules       Date:  2020-09-18       Impact factor: 4.411

5.  Discovery, Synthesis, and Optimization of Diarylisoxazole-3-carboxamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore.

Authors:  Sudeshna Roy; Justina Šileikytė; Marco Schiavone; Benjamin Neuenswander; Francesco Argenton; Jeffrey Aubé; Michael P Hedrick; Thomas D Y Chung; Michael A Forte; Paolo Bernardi; Frank J Schoenen
Journal:  ChemMedChem       Date:  2015-08-18       Impact factor: 3.466

  5 in total

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