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Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor |
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| Authors: | Jiang Cheng-Shi Zhou Rong Gong Jing-Xu Chen Li-Li Kurtán Tibor Shen Xu Guo Yue-Wei |
| Institution: | a State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China b East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, PR China c Department of Organic Chemistry, University of Debrecen, PO Box 20, 4010 Debrecen, Hungary |
| Abstract: | Macrolide (R)-de-O-methyllasiodiplodin (1), discovered to be a potent nonsteroidal antagonist of the mineralocorticoid receptor (MR), was synthesized via an efficient method and evaluated for MR antagonistic activity together with its analogs. Among all the tested compounds, compounds 18a, 18b and 18c, exhibited more potent antagonistic activity against MR with IC50 values ranging from 0.58 to 1.11 μM. Generally, it was obviously demonstrated that acetylation at phenolic hydroxyl groups and the ring size in analogs of 1 were very important for MR antagonist activity. |
| Keywords: | Macrolide (R)-De-O-methyllasiodiplodin Mineralocorticoid receptor Antagonist Ring-closing-metathesis reaction |
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