苯并噻唑类似物的抗疟活性：系统综述。

IF 2.1 4区医学 Q3 PHARMACOLOGY & PHARMACY

Fundamental & Clinical Pharmacology Pub Date : 2023-12-26 DOI:10.1111/fcp.12974

Linh Tran, Vo Linh Tu, Mohammad Najm Dadam, Jeza Muhamad Abdul Aziz, Tran Le Dinh Duy, Hajer Hatim Hassan Ahmed, Patrick Amanning Kwaah, Hoang Nghia Quoc, Truong Van Dat, Satoshi Mizuta, Kenji Hirayama, Nguyen Tien Huy

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引用次数: 0

摘要

背景：据报道，苯并噻唑衍生物具有广泛的生物活性，包括抗疟活性。本系统综述旨在总结和评估苯并噻唑类似物的抗疟活性：我们于 2017 年 10 月使用九个数据库进行了电子检索，随后于 2022 年 9 月进行了更新。我们不受限制地纳入了所有记录了含有苯并噻唑类似物的化合物抗疟活性的体外和体内原始研究。我们使用 ToxRTool 对每项纳入研究的偏倚风险进行了评估：我们的研究共纳入了 28 篇文章，这些文章或为体外研究，或为体内研究，或两者兼而有之。其中有 232 种物质被鉴定出对各种疟原虫菌株具有强效抗疟活性。苯并噻唑类似物显示出不同的抗疟机制，包括在体外研究中抑制恶性疟原虫酶，在体内研究中抑制血液中的寄生虫：结论：苯并噻唑衍生物是治疗疟疾的有效物质。结构-活性关系研究表明，苯并噻唑支架的取代模式在决定类似物的抗疟活性方面起着至关重要的作用。

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Antimalarial activities of benzothiazole analogs: A systematic review

Background

Benzothiazole derivatives have been reported to possess a wide range of biological activities, including antimalarial activity. This systematic review aims to summarize and evaluate the antimalarial activities of benzothiazole analogs.

Methods

We conducted an electronic search using nine databases in October 2017 and subsequently updated in September 2022. We included all original in vitro and in vivo studies that documented the antimalarial activities of compounds containing benzothiazole analogs with no restriction. The risk of bias of each included study was assessed by ToxRTool.

Results

Twenty-eight articles were included in our study, which are in vitro, in vivo, or both. Of these, 232 substances were identified to have potent antiplasmodial activity against various strains of the malaria parasite. Benzothiazole analogs show different antimalarial mechanisms, including inhibition of Plasmodium falciparum enzymes in in vitro studies and inhibition of blood parasites in in vivo studies.

Conclusions

Benzothiazole derivatives are promising substances for treating malaria. The structure–activity relationship studies suggest that the substitution pattern of the benzothiazole scaffold plays a crucial role in determining the antimalarial activity of the analog.

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来源期刊

Fundamental & Clinical Pharmacology 医学-药学

CiteScore

5.30

自引率

6.90%

发文量

111

审稿时长

6-12 weeks

期刊介绍： Fundamental & Clinical Pharmacology publishes reports describing important and novel developments in fundamental as well as clinical research relevant to drug therapy. Original articles, short communications and reviews are published on all aspects of experimental and clinical pharmacology including: Antimicrobial, Antiviral Agents Autonomic Pharmacology Cardiovascular Pharmacology Cellular Pharmacology Clinical Trials Endocrinopharmacology Gene Therapy Inflammation, Immunopharmacology Lipids, Atherosclerosis Liver and G-I Tract Pharmacology Metabolism, Pharmacokinetics Neuropharmacology Neuropsychopharmacology Oncopharmacology Pediatric Pharmacology Development Pharmacoeconomics Pharmacoepidemiology Pharmacogenetics, Pharmacogenomics Pharmacovigilance Pulmonary Pharmacology Receptors, Signal Transduction Renal Pharmacology Thrombosis and Hemostasis Toxicopharmacology Clinical research, including clinical studies and clinical trials, may cover disciplines such as pharmacokinetics, pharmacodynamics, pharmacovigilance, pharmacoepidemiology, pharmacogenomics and pharmacoeconomics. Basic research articles from fields such as physiology and molecular biology which contribute to an understanding of drug therapy are also welcomed.