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Published on: May 21, 2018
Recent Developments of Coumarin Hybrids as Anti-fungal Agents
Xin-Liang Hu1, Zhi Xu2, Ming-Liang Liu3
1School of Chemistry and Materials Science, Hubei Engineering University, Xiaogan, Hubei, China.
Abstract:
Fungi place a huge burden on global healthcare systems attributed to the fact that fungal infections are responsible for the high morbidity and mortality rates in patients who received stem cell transplantation, antineoplastic chemotherapy, organ transplants or suffered Human Immunodeficiency Virus (HIV) infection. Unfortunately, almost none of the representative anti-fungal agents currently used in clinical therapy are ideal in terms of efficacy, anti-fungal spectrum or safety. Moreover, the rapid development of resistance to existing anti-fungal drugs has further aggravated the mortality and spread of fungi, creating an urgent need for novel anti-fungal agents. The broad spectrum of biological activities and successful usage in clinic made coumarins a promising anti-fungal candidate. Furthermore, hybridization of other pharmacophores with coumarin motif may enhance the anti-fungal efficacy, broaden the anti-fungal spectrum and improve the safety profiles. Thus, numerous coumarin hybrids have been assessed for their anti-fungal activities, and some of them showed promising potency and may have a novel mechanism of action. This review aims to outline the recent development of coumarin hybrids as potential anti-fungal agents and summarize their Structure-Activity Relationship (SAR) to provide an insight for rational designs of more active agents.
Insights
Novel coumarin hybrids show promise as effective antifungal agents, addressing the urgent need for new treatments due to drug resistance and limited options. Their development offers potential for improved efficacy and safety in combating fungal infections.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Mycology
Background:
- Fungal infections pose significant global health challenges, leading to high morbidity and mortality, particularly in immunocompromised patients.
- Current antifungal therapies exhibit limitations in efficacy, spectrum, and safety, compounded by the rise of drug-resistant fungal strains.
- There is an urgent clinical need for novel antifungal agents with improved profiles.
Purpose of the Study:
- To review recent advancements in the development of coumarin hybrids as potential antifungal agents.
- To summarize the Structure-Activity Relationships (SAR) of these compounds.
- To provide insights for the rational design of new, more potent antifungal agents.
Main Methods:
- Literature review of studies assessing coumarin hybrids for antifungal activity.
- Analysis of Structure-Activity Relationships (SAR) to identify key structural features influencing efficacy.
- Evaluation of reported antifungal spectrum, potency, and safety profiles.
Main Results:
- Coumarins demonstrate broad-spectrum biological activities and have been successfully used in clinical settings, making them promising antifungal scaffolds.
- Hybridization of coumarin motifs with other pharmacophores has yielded compounds with enhanced antifungal efficacy, broader spectrum, and improved safety.
- Several coumarin hybrids have exhibited promising antifungal potency, with some suggesting novel mechanisms of action.
Conclusions:
- Coumarin hybrids represent a promising class of compounds for the development of novel antifungal agents.
- Understanding the SAR of coumarin hybrids is crucial for designing next-generation antifungals.
- Further research into coumarin hybrids could lead to effective treatments for challenging fungal infections.
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