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dc.contributor.authorWoo, Hyun Min-
dc.contributor.authorLee, Yun Suk-
dc.contributor.authorRoh, Eun Joo-
dc.contributor.authorSeo, Seon Hee-
dc.contributor.authorSong, Chi Man-
dc.contributor.authorChung, Hye Jin-
dc.contributor.authorPae, Ae Nim-
dc.contributor.authorShin, Kye Jung-
dc.date.accessioned2024-01-20T16:03:55Z-
dc.date.available2024-01-20T16:03:55Z-
dc.date.created2021-09-05-
dc.date.issued2011-10-01-
dc.identifier.issn0960-894X-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/129905-
dc.description.abstractTo obtain selective and potent inhibitor for T-type calcium channel by ligand based drug design, 4-piperidinecarboxylate and 4-piperidinecyanide derivatives were prepared and evaluated for in vitro and in vivo activity against alpha(1G) calcium channel. Among them, several compounds showed good T-type calcium channel inhibitory activity and minimal off-target activity over hERG channel (% inhibition at 10 mu M = 61.85-71.99, hERG channel IC50 = 1.57 +/- 0.14-4.98 +/- 0.36 mu M). Selected compound 31a was evaluated on SNL model of neuropathic pain and showed inhibitory effect on mechanical allodynia. (C) 2011 Elsevier Ltd. All rights reserved.-
dc.languageEnglish-
dc.publisherPergamon Press Ltd.-
dc.subjectCA2+ CHANNELS-
dc.subjectMIBEFRADIL-
dc.subjectDISCOVERY-
dc.titleSynthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers-
dc.typeArticle-
dc.identifier.doi10.1016/j.bmcl.2011.07.087-
dc.description.journalClass1-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry Letters, v.21, no.19, pp.5910 - 5915-
dc.citation.titleBioorganic & Medicinal Chemistry Letters-
dc.citation.volume21-
dc.citation.number19-
dc.citation.startPage5910-
dc.citation.endPage5915-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000294714400054-
dc.identifier.scopusid2-s2.0-80052555689-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.type.docTypeArticle-
dc.subject.keywordPlusCA2+ CHANNELS-
dc.subject.keywordPlusMIBEFRADIL-
dc.subject.keywordPlusDISCOVERY-
dc.subject.keywordAuthorT-type calcium channel-
dc.subject.keywordAuthorNeuropathic pain-
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