Issue 7, 2020

A practical synthesis of amino limonin/deoxylimonin derivatives as effective mitigators against inflammation and nociception

Abstract

A practical synthetic route, consisting of 5 steps, has been developed and applied successfully for converting limonin/deoxylimonin into the corresponding amino derivatives I-5aI-5e and II-5aII-5e. Deoxylimonin analogs II-5a and II-5b bearing an open A ring structure underwent ring closure reaction by employing the Mitsunobu procedure to afford II-6a and II-6b. All of the 12 newly synthesized compounds were subjected to preliminary screening for evaluating their inflammation and nociception inhibition efficacy. The most promising compounds, I-5b and II-5d, were selected for further investigation by a carrageenan-induced mouse paw edema model, both of which displayed a dose–response dependent manner and demonstrated superior anti inflammation capacity to that of indomethacin in the first 2 hours.

Graphical abstract: A practical synthesis of amino limonin/deoxylimonin derivatives as effective mitigators against inflammation and nociception

Supplementary files

Article information

Article type
Research Article
Submitted
12 Apr 2020
Accepted
12 May 2020
First published
16 Jun 2020

RSC Med. Chem., 2020,11, 843-847

A practical synthesis of amino limonin/deoxylimonin derivatives as effective mitigators against inflammation and nociception

S. Wang, X. Han, Y. Yang, R. Chen, Z. Guo, Q. Zhu and Y. Xu, RSC Med. Chem., 2020, 11, 843 DOI: 10.1039/D0MD00117A

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