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硫代色烯和硫代色满：对其多样生物活性及构效关系（SAR）见解的全面综述

Thiochromenes and thiochromanes: a comprehensive review of their diverse biological activities and structure-activity relationship (SAR) insights.

作者信息

Murugappan Solai, Kirad Shivani, Ala Chandu, Kuthe Pranali Vijaykumar, Kondapalli Chandra Sekhar Venkata Gowri, Sankaranarayanan Murugesan

机构信息

Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science Pilani Pilani Campus, Vidya Vihar Pilani-333031 Rajasthan India

Department of Chemistry, Birla Institute of Technology and Science Pilani Hyderabad Campus, Jawahar Nagar, Kapra Mandal Hyderabad-500078 Telangana India.

出版信息

RSC Med Chem. 2025 Mar 24;16(5):1941-1968. doi: 10.1039/d4md00995a. eCollection 2025 May 22.

DOI:10.1039/d4md00995a
PMID:40135146
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11931433/
Abstract

Thiochromene and thiochromane scaffolds, sulfur containing heterocycles, have gained significant attention in medicinal chemistry due to their diverse pharmacological activities. This review provides a comprehensive analysis of their antibacterial, antifungal, antiviral, anti-parasitic, and anticancer properties, emphasizing their therapeutic potential. SAR studies highlight key molecular modifications such as electron withdrawing substituents, sulfur oxidation, and tailored ring substitutions that enhance bioactivity, potency, and target specificity. Mechanistic insights reveal their ability to inhibit microbial enzymes, disrupt cellular pathways, and modulate key biological targets. By summarizing recent advancements, this review underscores the potential of thiochromene and thiochromane based therapeutics and encourages further research to address existing limitations and enhance their drug development prospects.

摘要

硫代色烯和硫代色满骨架，即含硫杂环化合物，因其多样的药理活性而在药物化学领域受到了广泛关注。本综述对它们的抗菌、抗真菌、抗病毒、抗寄生虫和抗癌特性进行了全面分析，强调了它们的治疗潜力。构效关系研究突出了关键的分子修饰，如吸电子取代基、硫氧化以及经过定制的环取代，这些修饰可增强生物活性、效力和靶标特异性。作用机制研究揭示了它们抑制微生物酶、破坏细胞通路以及调节关键生物靶标的能力。通过总结近期进展，本综述强调了基于硫代色烯和硫代色满的治疗方法的潜力，并鼓励进一步开展研究以解决现有局限性并提升其药物开发前景。

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本文引用的文献

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Chem Biodivers. 2024 Feb;21(2):e202301738. doi: 10.1002/cbdv.202301738. Epub 2024 Jan 12.
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The Role of Five-Membered Heterocycles in the Molecular Structure of Antibacterial Drugs Used in Therapy.五元杂环在治疗用抗菌药物分子结构中的作用。
Pharmaceutics. 2023 Oct 29;15(11):2554. doi: 10.3390/pharmaceutics15112554.
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Discovery of C-3 isoxazole substituted thiochromone S,S-dioxide derivatives as potent and selective inhibitors for monoamine oxidase B (MAO-B).发现 C-3 异噁唑取代硫代色酮 S，S-二氧化物衍生物是强效和选择性的单胺氧化酶 B（MAO-B）抑制剂。
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A novel alpha-amylase inhibitor-based spirooxindole-pyrrolidine-clubbed thiochromene-pyrzaole pharmacophores: Unveiling the [3+2] cycloaddition reaction by molecular electron density theory.一种基于新型α-淀粉酶抑制剂的螺环氧化吲哚-吡咯烷-结合硫代色烯-吡唑药效团：通过分子电子密度理论揭示[3+2]环加成反应
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