A Practical Synthesis of Amino Limonin/deoxylimonin Derivatives As Effective Mitigators Against Inflammation and Nociception

Overview

Journal RSC Med Chem

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2021 Jan 22

PMID 33479680

Citations 1

Authors

Shaochi Wang

Xueqing Han

Yun Yang

Rui Chen

Zhaoyi Guo

Qihua Zhu

Yungen Xu

Affiliations

Soon will be listed here.

Abstract

A practical synthetic route, consisting of 5 steps, has been developed and applied successfully for converting limonin/deoxylimonin into the corresponding amino derivatives - and - . Deoxylimonin analogs and bearing an open A ring structure underwent ring closure reaction by employing the Mitsunobu procedure to afford and . All of the 12 newly synthesized compounds were subjected to preliminary screening for evaluating their inflammation and nociception inhibition efficacy. The most promising compounds, and , 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.

Citing Articles

Preclinical Drug Pharmacokinetic, Tissue Distribution and Excretion Profiles of the Novel Limonin Derivate HY-071085 as an Anti-Inflammatory and Analgesic Candidate in Rats and Beagle Dogs.

Dong L, Liu W, Zhao X, Yu F, Xu Y, Su M Pharmaceuticals (Basel). 2022; 15(7).

PMID: 35890101 PMC: 9316000. DOI: 10.3390/ph15070801.

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