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Synthesis of PPAR-.Activators Inspired by the Marine Natural Product, Paecilocin Aopen access
- Authors
- Xiao, B[Xiao, Bin]; Su, MZ[Su, Mingzhi]; Kim, EL[Kim, Eun La]; Hong, JK[Hong, Jongki]; Chung, HY[Chung, Hae Young]; Kim, HS[Kim, Hyung Sik]; Yin, J[Yin, Jun]; Jung, JH[Jung, Jee H.]
- Issue Date
- Feb-2014
- Publisher
- MDPI AG
- Keywords
- PPAR-; diabetes; phthalimide; luciferase assay; docking simulation; cell proliferation
- Citation
- MARINE DRUGS, v.12, no.2, pp.926 - 939
- Indexed
- SCIE
SCOPUS
- Journal Title
- MARINE DRUGS
- Volume
- 12
- Number
- 2
- Start Page
- 926
- End Page
- 939
- ISSN
- 1660-3397
- Abstract
- A series of N-substituted phthalimide derivatives were synthesized based on a pharmacophore study of paecilocin A (a natural PPAR- agonist) and synthetic leads. The introduction of hydrophilic and hydrophobic groups to the phthalimide skeleton yielded compounds 3-14. Compound 7 showed significant PPAR- activation in a luciferase assay using rat liver Ac2F cells. Docking simulations showed that a free hydroxyl group on the phthalimide head and a suitable hydrophilic tail, including a phenyl linker, were beneficial for PPAR- activation. Compound 7 and rosiglitazone concentration-dependently activated PPAR- with EC50 values of 0.67 M and 0.028 M, respectively. These phthalimide derivatives could be further investigated as a new class of PPAR- ligands.
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Collections - Pharmacy > Department of Pharmacy > 1. Journal Articles
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