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Metabolic syndrome, which refers to a group of abnormalities that occur together and increase the risk of coronary artery disease, stroke, type 2 diabetes, and cachexia, can be treated using <jats:styled-content style=\"fixed-case\">ATGL<\/jats:styled-content>\u2010specific inhibitors. Atglistatin (<jats:bold>1<\/jats:bold>) is the first small\u2010molecule inhibitor of <jats:styled-content style=\"fixed-case\">ATGL<\/jats:styled-content>. In this study, we designed and synthesized 29 Atglistatin derivatives and evaluated their inhibition of forskolin\u2010stimulated lipolysis in 3T3\u2010L1 adipocytes as an indicator of their potential to inhibit <jats:styled-content style=\"fixed-case\">ATGL<\/jats:styled-content> in adipose tissues. Among all the tested Atglistatin analogs, we previously found that the thiourea compound <jats:bold>9e<\/jats:bold> showed potent <jats:styled-content style=\"fixed-case\">ATGL<\/jats:styled-content> inhibitory activity in vitro, which was much stronger than that of Atglistatin, and its inhibitory activity in vivo was similar to that of Atglistatin. This tool compound could be used to study the pathophysiology and druggability of <jats:styled-content style=\"fixed-case\">ATGL<\/jats:styled-content> in animal models of metabolic disease and cachexia.<\/jats:p>","DOI":"10.1111\/cbdd.13029","type":"journal-article","created":{"date-parts":[[2017,5,26]],"date-time":"2017-05-26T09:18:43Z","timestamp":1495790323000},"page":"1122-1133","source":"Crossref","is-referenced-by-count":8,"title":["Design and synthesis of Atglistatin derivatives as adipose triglyceride lipase inhibitors"],"prefix":"10.1111","volume":"90","author":[{"given":"Jiyu","family":"Jin","sequence":"first","affiliation":[{"name":"School of Chemistry and Molecular Engineering East China Normal University  Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Suling","family":"Huang","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences  Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lei","family":"Wang","sequence":"additional","affiliation":[{"name":"School of Chemistry and Molecular Engineering East China Normal University  Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ying","family":"Leng","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences  Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3041-9200","authenticated-orcid":false,"given":"Wei","family":"Lu","sequence":"additional","affiliation":[{"name":"School of Chemistry and Molecular Engineering East China Normal University  Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2017,6,26]]},"reference":[{"key":"e_1_2_6_2_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.1100747"},{"key":"e_1_2_6_3_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.M403855200"},{"key":"e_1_2_6_4_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.M407841200"},{"key":"e_1_2_6_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2016.04.021"},{"key":"e_1_2_6_6_1","doi-asserted-by":"publisher","DOI":"10.1210\/en.2010-0661"},{"key":"e_1_2_6_7_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.M109.047787"},{"key":"e_1_2_6_8_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.1198973"},{"key":"e_1_2_6_9_1","doi-asserted-by":"publisher","DOI":"10.1093\/cvr\/cvt124"},{"key":"e_1_2_6_10_1","first-page":"17","volume":"2011","author":"Haemmerle G.","journal-title":"Nat. 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