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제123회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Synthesis and recent updates on thiazoline containing agonists of selective peroxisome proliferator-activated receptor δ

2019년 2월 14일 14시 48분 04초
MEDI.P-418 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
4월 18일 (목요일) 11:00~12:30
Medicinal Chemistry
저자 및
Tara Man Kadayat, Su-Jeong Lee, Sung Jin Cho*, Jungwook Chin*
New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Korea
Peroxisome proliferator-activated receptors (PPARs) are members of ligand-activated transcription factors of the nuclear receptor family. Based on distinct ligand specificity, physiological roles and tissue distribution, PPARs are classified into three isotypes namely PPARa, PPARg, and PPARδ. PPARδ is considered as a promising biological target for the development of new drugs to treat metabolic syndrome including hyperlipidemia. As part of our continuous effort to develop new analogues of GW501516 (a well-known selective and potent PPARδ agonist), we introduced a facile method for the synthesis of new thiazoline containing intermediate for the preparation of novel PPARδ-selective agonists. The synthetic method used is short and convenient as it did not require the use of extreme conditions such as -78 °C. In this study, we developed efficient route for the synthesis of distinctive thiazoline containing compounds as selective PPARδ agonists. These reaction conditions and unique key intermediate may be applicable for the synthesis of other related pharmaceuticals. The preliminary in vitro PPARδ activity of synthesized compounds demonstrates this unique thiazoline core containing compounds as potential PPARδ –selective agonist. In addition to this synthetic work, recent updates on selective agonists of PPARδ will also be described.