Peripheral Selective Oxadiazolylphenyl Alanine Derivatives as Tryptophan Hydroxylase 1 Inhibitors for Obesity and Fatty Liver Disease

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dc.contributor.authorBae, Eun Jungko
dc.contributor.authorChoi, Won Gunko
dc.contributor.authorPagire, Haushabhau S.ko
dc.contributor.authorPagire, Suvarna H.ko
dc.contributor.authorParameswaran, Saravananko
dc.contributor.authorChoi, Jun-Hoko
dc.contributor.authorYoon, Jihyeonko
dc.contributor.authorChoi, Won-ilko
dc.contributor.authorLee, Ji Hunko
dc.contributor.authorSong, Jin Sookko
dc.contributor.authorBae, Myung Aeko
dc.contributor.authorKim, Mijinko
dc.contributor.authorJeon, Jae-Hanko
dc.contributor.authorLee, In-Kyuko
dc.contributor.authorKim, Hailko
dc.contributor.authorAhn, Jin Heeko
dc.date.accessioned2021-03-17T06:51:03Z-
dc.date.available2021-03-17T06:51:03Z-
dc.date.created2021-03-17-
dc.date.created2021-03-17-
dc.date.issued2021-01-
dc.identifier.citationJOURNAL OF MEDICINAL CHEMISTRY, v.64, no.2, pp.1037 - 1053-
dc.identifier.issn0022-2623-
dc.identifier.urihttp://hdl.handle.net/10203/281636-
dc.description.abstractTryptophan hydroxylase 1 (TPH1) has been recently suggested as a promising therapeutic target for treating obesity and fatty liver disease. A new series of 1,2,4-oxadiazolylphenyl alanine derivatives were identified as TPH1 inhibitors. Among them, compound 23a was the most active in vitro, with an IC50 (half-maximal inhibitory concentration) value of 42 nM, showed good liver microsomal stability, and showed no significant inhibition of CYP and hERG. Compound 23a inhibited TPH1 in the peripheral tissue with limited BBB penetration. In high-fat diet-fed mice, 23a reduced body weight gain, body fat, and hepatic lipid accumulation. Also, 23a improved glucose intolerance and energy expenditure. Taken together, compound 23a shows promise as a therapeutic agent for the treatment of obesity and fatty liver diseases.-
dc.languageEnglish-
dc.publisherAMER CHEMICAL SOC-
dc.titlePeripheral Selective Oxadiazolylphenyl Alanine Derivatives as Tryptophan Hydroxylase 1 Inhibitors for Obesity and Fatty Liver Disease-
dc.typeArticle-
dc.identifier.wosid000614306000010-
dc.identifier.scopusid2-s2.0-85100143819-
dc.type.rimsART-
dc.citation.volume64-
dc.citation.issue2-
dc.citation.beginningpage1037-
dc.citation.endingpage1053-
dc.citation.publicationnameJOURNAL OF MEDICINAL CHEMISTRY-
dc.identifier.doi10.1021/acs.jmedchem.0c01560-
dc.contributor.localauthorKim, Hail-
dc.contributor.nonIdAuthorBae, Eun Jung-
dc.contributor.nonIdAuthorPagire, Haushabhau S.-
dc.contributor.nonIdAuthorPagire, Suvarna H.-
dc.contributor.nonIdAuthorParameswaran, Saravanan-
dc.contributor.nonIdAuthorChoi, Jun-Ho-
dc.contributor.nonIdAuthorYoon, Jihyeon-
dc.contributor.nonIdAuthorLee, Ji Hun-
dc.contributor.nonIdAuthorSong, Jin Sook-
dc.contributor.nonIdAuthorBae, Myung Ae-
dc.contributor.nonIdAuthorKim, Mijin-
dc.contributor.nonIdAuthorJeon, Jae-Han-
dc.contributor.nonIdAuthorLee, In-Kyu-
dc.contributor.nonIdAuthorAhn, Jin Hee-
dc.description.isOpenAccessN-
dc.type.journalArticleArticle-
dc.subject.keywordPlusSEROTONIN SYNTHESIS-
dc.subject.keywordPlusPARA-CHLOROPHENYLALANINE-
dc.subject.keywordPlusP-CHLOROPHENYLALANINE-
dc.subject.keywordPlusDISCOVERY-
dc.subject.keywordPlusTARGET-
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