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dc.contributor.authorJung, HK-
dc.contributor.authorDoddareddy, MR-
dc.contributor.authorCha, JH-
dc.contributor.authorRhim, H-
dc.contributor.authorCho, YS-
dc.contributor.authorKoh, HY-
dc.contributor.authorJung, BY-
dc.contributor.authorPae, AN-
dc.date.accessioned2024-01-21T06:36:09Z-
dc.date.available2024-01-21T06:36:09Z-
dc.date.created2021-09-04-
dc.date.issued2004-08-01-
dc.identifier.issn0968-0896-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/137322-
dc.description.abstractA small molecule library of piperazinylalkylisoxazole derivatives containing about 600 compounds was designed, synthesized and evaluated for blocking effects on T-type Ca2+ channel. Several ligands were identified to possess high inhibitory activity against the T-type Ca2+ channel. The compound 21 with trifluoromethyl substituents at C-3-position of phenyl group (W) and C-2-position of phenyl group (R-2) showed the highest inhibitory activity with IC50 value of 1.02 muM, which is comparable to that of mibefradil. (C) 2004 Elsevier Ltd. All rights reserved.-
dc.languageEnglish-
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD-
dc.subjectCALCIUM-CHANNELS-
dc.subjectRECEPTOR LIGANDS-
dc.subjectCLONED HUMAN-
dc.subjectDOPAMINE-
dc.subjectANTAGONIST-
dc.subjectINHIBITION-
dc.subjectEFFICACY-
dc.subjectCURRENTS-
dc.subjectAGONIST-
dc.subjectDESIGN-
dc.titleSynthesis and biological evaluation of novel T-type Ca2+ channel blockers-
dc.typeArticle-
dc.identifier.doi10.1016/j.bmc.2004.06.011-
dc.description.journalClass1-
dc.identifier.bibliographicCitationBIOORGANIC & MEDICINAL CHEMISTRY, v.12, no.15, pp.3965 - 3970-
dc.citation.titleBIOORGANIC & MEDICINAL CHEMISTRY-
dc.citation.volume12-
dc.citation.number15-
dc.citation.startPage3965-
dc.citation.endPage3970-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000222886700001-
dc.identifier.scopusid2-s2.0-3042831495-
dc.relation.journalWebOfScienceCategoryBiochemistry & Molecular Biology-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.relation.journalResearchAreaBiochemistry & Molecular Biology-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.type.docTypeArticle-
dc.subject.keywordPlusCALCIUM-CHANNELS-
dc.subject.keywordPlusRECEPTOR LIGANDS-
dc.subject.keywordPlusCLONED HUMAN-
dc.subject.keywordPlusDOPAMINE-
dc.subject.keywordPlusANTAGONIST-
dc.subject.keywordPlusINHIBITION-
dc.subject.keywordPlusEFFICACY-
dc.subject.keywordPlusCURRENTS-
dc.subject.keywordPlusAGONIST-
dc.subject.keywordPlusDESIGN-
dc.subject.keywordAuthorT-type calcium channel-
dc.subject.keywordAuthorsynthesis-
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