文献检索文档翻译深度研究
Suppr Zotero 插件Zotero 插件
邀请有礼套餐&价格历史记录

新学期,新优惠

限时优惠:9月1日-9月22日

30天高级会员仅需29元

1天体验卡首发特惠仅需5.99元

了解详情
不再提醒
插件&应用
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
高级版
套餐订阅购买积分包
AI 工具
文献检索文档翻译深度研究
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2025

In vitro Assessment of Camphor Hydrazone Derivatives as an Agent Against Leishmania amazonensis.

作者信息

da Silva Emerson Teixeira, de Andrade Gabriel Fernandes, Araújo Adriele da Silva, Almeida Ayla das Chagas, Coimbra Elaine S, de Souza Marcus Vinícius Nora

机构信息

Fundação Oswaldo Cruz (Fiocruz), Instituto de Tecnologia em Fármacos Farmanguinhos, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro, 21041-250, Brazil.

Instituto de Química, Universidade Federal do Rio de Janeiro, Av. Brigadeiro Trompowsky, Rio de Janeiro, 21044-020, Brazil.

出版信息

Acta Parasitol. 2020 Mar;65(1):203-207. doi: 10.2478/s11686-019-00146-5. Epub 2019 Dec 12.


DOI:10.2478/s11686-019-00146-5
PMID:31832921
Abstract

PURPOSE: Due to serious problems with the treatment of leishmaniasis all around the world, here is an urgent need in the search for new drugs that are more effective and safer for the treatment of the various forms of leishmaniasis. Actual therapy is limited and lacks sufficient efficacy due to incomplete elimination of the parasites form of patients. In this sense, we decided to evaluate, by first-time, a series of seventeen camphor hydrazone derivatives (2a-2p) against Leishmania amazonensis. METHODS: The compounds previously synthesized from camphor, an abundant natural compound, were evaluated in vitro against the extra and intracellular forms of Leishmania amazonensis, and murine macrophages. RESULTS: The majority of compounds, fourteen, displayed activity against the intracellular form of the parasite (amastigote) with IC values ranging from 21.78 to 58.23 µM, being six compounds active for both forms of the parasite. The compound 2i exhibited higher activity against the amastigote form with the value of IC (21.78 µM) close to standard utilized miltefosine (12.74 µM) and selectivity index of at least 6.9. Six compounds displayed activity against promastigote form of Leishmania amazonensis 2g, 2j-2n (41.17-69.59 µM), with the compound 2m being the more active with IC = 41.17 µM, 1.9 times less active than the reference drug (IC = 21.39 µM). The compound 2m was the more selective to this form, with a selectivity index of at least 3.6. All the compounds were non-cytotoxic to macrophages. CONCLUSIONS: Most compounds showed activity against amastigote form of Leishmania amazonensis, being that they were not cytotoxic to macrophage at the maximum tested concentration, showing the selective property of these compounds. Since amastigotes are the parasite stages that cause the disease in humans, these results highlight the antileishmanial effect of the compounds. This study indicates the possible development of candidates to leishmanicidal drugs from an abundant natural compound of easy access.

摘要

相似文献

[1]
In vitro Assessment of Camphor Hydrazone Derivatives as an Agent Against Leishmania amazonensis.

Acta Parasitol. 2020-3

[2]
Aminoquinoline compounds: Effect of 7-chloro-4-quinolinylhydrazone derivatives against Leishmania amazonensis.

Exp Parasitol. 2016-12

[3]
In vitro evaluation of (-)α-bisabolol as a promising agent against Leishmania amazonensis.

Exp Parasitol. 2015-1

[4]
Antileishmanial activity of cordiaquinone E towards Leishmania (Leishmania) amazonensis.

Int Immunopharmacol. 2021-1

[5]
Semicarbazone derivatives as promising therapeutic alternatives in leishmaniasis.

Exp Parasitol. 2019-6

[6]
In Vitro and In Vivo Antileishmanial Activity of Thioridazine.

Acta Parasitol. 2024-3

[7]
Evaluation of the in vitro and in vivo antileishmanial activity of a chloroquinolin derivative against Leishmania species capable of causing tegumentary and visceral leishmaniasis.

Exp Parasitol. 2019-4

[8]
Antileishmanial activity of a naphthoquinone derivate against promastigote and amastigote stages of Leishmania infantum and Leishmania amazonensis and its mechanism of action against L. amazonensis species.

Parasitol Res. 2018-2

[9]
Leishmanicidal activity of Piper marginatum Jacq. from Santarém-PA against Leishmania amazonensis.

Exp Parasitol. 2020-1-28

[10]
Efficacy of a Binuclear Cyclopalladated Compound Therapy for Cutaneous Leishmaniasis in the Murine Model of Infection with Leishmania amazonensis and Its Inhibitory Effect on Topoisomerase 1B.

Antimicrob Agents Chemother. 2017-7-25

引用本文的文献

[1]
The Beneficial Use of , Artemisinin, and Other Compounds in Animal Health.

Animals (Basel). 2025-5-8

[2]
Drug Discovery for Cutaneous Leishmaniasis: A Review of Developments in the Past 15 Years.

Microorganisms. 2023-11-23

[3]
Examination of the Topical Effect of the Combination of and Vinegar on the Improvement of Rural Cutaneous Leishmaniasis Lesions.

Adv Biomed Res. 2023-2-25

[4]
1,4-Disubstituted-1,2,3-Triazole Compounds Induce Ultrastructural Alterations in Promastigote: An in Vitro Antileishmanial and in Silico Pharmacokinetic Study.

Int J Mol Sci. 2020-9-18

本文引用的文献

[1]
Synthesis of Camphor-Derived Bis(pyrazolylpyridine) Rhodium(III) Complexes: Structure-Reactivity Relationships and Biological Activity.

Inorg Chem. 2018-12-19

[2]
Leishmaniasis.

Lancet. 2018-8-17

[3]
Synthesis, Biological Activity, and Mechanism of Action of 2-Pyrazyl and Pyridylhydrazone Derivatives, New Classes of Antileishmanial Agents.

ChemMedChem. 2018-6-21

[4]
Synthesis of alkynyl-substituted camphor derivatives and their use in the preparation of paclitaxel-related compounds.

Beilstein J Org Chem. 2017-6-26

[5]
Camphor--a fumigant during the Black Death and a coveted fragrant wood in ancient Egypt and Babylon--a review.

Molecules. 2013-5-10

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

推荐工具

医学文档翻译智能文献检索