4.5 Review

Evolution of chromone-like compounds as potential antileishmanial agents, through the 21stcentury

Journal

EXPERT OPINION ON DRUG DISCOVERY
Volume 15, Issue 12, Pages 1425-1439

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/17460441.2020.1801630

Keywords

Chromones; structure-activity relationship; antileishmanial agents; leishmaniaspecies; arginase; nucleoside hydrolase

Funding

  1. Fundacao para a Ciencia e a Tecnologia (FCT)/Ministry of Science and Technology, Portugal (MCT)
  2. FEDER through QOPNA [FCT UID/QUI/00062/2019, LAQV-REQUIMTE UIDB/50006/2020]
  3. FCT [PD/BD/135103/2017]
  4. Fundação para a Ciência e a Tecnologia [PD/BD/135103/2017] Funding Source: FCT

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Introduction Leishmaniasis is one of the most neglected diseases of modern times that mainly affects people from developing countries, with approximately 350 million people considered at risk of developing leishmaniasis. Therefore, the development of novel antileishmanial treatments is becoming the focus of numerous research groups, with the support of the World Health Organization, which hopes to eradicate this disease in the near future. Areas covered This review focuses on the interest of chromones for the development of future treatments against leishmaniasis. In addition to plant-based chromone derivatives, structure-activity relationship studies that aim to identify the optimal structural features of the chromones' antileishmanial activity are also described and discussed. Expert opinion The numerous examples of chromones depicted in this paper, allied with the SAR studies presented herein, suggest that the chromone scaffold is a privileged core for the design and development of novel antileishmanial agents. However, some concerns have been raised concerning the considerable variability observed in the results throughout the scientific bibliography. These inconsistencies may explain the absence of pharmacodynamic and pharmacokinetic studies as well as clinical trials.

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