دورية أكاديمية

Scaffold-Hopping Strategies in Aurone Optimization: A Comprehensive Review of Synthetic Procedures and Biological Activities of Nitrogen and Sulfur Analogues

التفاصيل البيبلوغرافية
العنوان: Scaffold-Hopping Strategies in Aurone Optimization: A Comprehensive Review of Synthetic Procedures and Biological Activities of Nitrogen and Sulfur Analogues
المؤلفون: Gabriele La Monica, Federica Alamia, Alessia Bono, Antonino Lauria, Annamaria Martorana
المصدر: Molecules, Vol 29, Iss 12, p 2813 (2024)
بيانات النشر: MDPI AG, 2024.
سنة النشر: 2024
المجموعة: LCC:Organic chemistry
مصطلحات موضوعية: aurones, scaffold hopping, biological activities, organic synthesis, azaaurones, thioaurones, Organic chemistry, QD241-441
الوصف: Aurones, particular polyphenolic compounds belonging to the class of minor flavonoids and overlooked for a long time, have gained significative attention in medicinal chemistry in recent years. Indeed, considering their unique and outstanding biological properties, they stand out as an intriguing reservoir of new potential lead compounds in the drug discovery context. Nevertheless, several physicochemical, pharmacokinetic, and pharmacodynamic (P3) issues hinder their progression in more advanced phases of the drug discovery pipeline, making lead optimization campaigns necessary. In this context, scaffold hopping has proven to be a valuable approach in the optimization of natural products. This review provides a comprehensive and updated picture of the scaffold-hopping approaches directed at the optimization of natural and synthetic aurones. In the literature analysis, a particular focus is given to nitrogen and sulfur analogues. For each class presented, general synthetic procedures are summarized, highlighting the key advantages and potential issues. Furthermore, the biological activities of the most representative scaffold-hopped compounds are presented, emphasizing the improvements achieved and the potential for further optimization compared to the aurone class.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 29122813
1420-3049
Relation: https://www.mdpi.com/1420-3049/29/12/2813; https://doaj.org/toc/1420-3049
DOI: 10.3390/molecules29122813
URL الوصول: https://doaj.org/article/2560a09736724409adc48b7ae8e6dd47
رقم الأكسشن: edsdoj.2560a09736724409adc48b7ae8e6dd47
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:29122813
14203049
DOI:10.3390/molecules29122813