Amine-Linked Flavonoids As Agents Against Cutaneous Leishmaniasis

Overview

Journal Antimicrob Agents Chemother

Publisher American Society for Microbiology

Specialty Pharmacology

Date 2021 Mar 9

PMID 33685890

Citations 2

Authors

Chin-Fung Chan

Zhen Liu

Iris L K Wong

Xianliang Zhao

Zaofeng Yang

Jiale Zheng

Marianne M Lee

Michael K Chan

Tak Hang Chan

Larry M C Chow

Affiliations

Soon will be listed here.

Abstract

We have designed, synthesized, and characterized a library of 38 novel flavonoid compounds linked with amines. Some of these amine-linked flavonoids have potent activity against parasites that cause cutaneous leishmaniasis, a tropical disease endemic in 80 countries worldwide. The most promising candidate, , was highly active with IC of 0.3 μM against , and amastigotes. It was metabolically stable (39% and 66% of remaining after 30-minute incubation with human and rat liver microsomes respectively). In LV78 cutaneous leishmaniasis mouse model, intralesional injection of (10 mg/kg, once every 4 days for 8 times) demonstrated promising effect in reducing the footpad lesion thickness by 72%, displaying an efficacy comparable to SSG (63%).

Citing Articles

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Surur A, Chan C, Bartz F, Wong I, Nguyen V, Schulig L RSC Med Chem. 2024; .

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