Scaffold-Hopping Strategies in Aurone Optimization: A Comprehensive Review of Synthetic Procedures and Biological Activities of Nitrogen and Sulfur Analogues DOI Creative Commons
Gabriele La Monica, Federica Alamia, Alessia Bono

и другие.

Molecules, Год журнала: 2024, Номер 29(12), С. 2813 - 2813

Опубликована: Июнь 13, 2024

Aurones, particular polyphenolic compounds belonging to the class of minor flavonoids and overlooked for a long time, have gained significative attention in medicinal chemistry recent years. Indeed, considering their unique outstanding biological properties, they stand out as an intriguing reservoir new potential lead drug discovery context. Nevertheless, several physicochemical, pharmacokinetic, pharmacodynamic (P3) issues hinder progression more advanced phases pipeline, making optimization campaigns necessary. In this context, scaffold hopping has proven be valuable approach natural products. This review provides comprehensive updated picture scaffold-hopping approaches directed at synthetic aurones. literature analysis, focus is given nitrogen sulfur analogues. For each presented, general procedures are summarized, highlighting key advantages issues. Furthermore, activities most representative scaffold-hopped emphasizing improvements achieved further compared aurone class.

Язык: Английский

Transition-metal-free regioselective synthesis of spiro-oxazolidines through [3 + 2] annulation reactions of azadienes with haloalcohols DOI Creative Commons

Amol T. Savekar,

Sonali M. Vitnor,

Vishal B. Karande

и другие.

RSC Advances, Год журнала: 2025, Номер 15(14), С. 10634 - 10638

Опубликована: Янв. 1, 2025

The transition-metal-free regioselective [3 + 2] annulation of azadienes with haloalcohols for the preparation highly functionalized spiro-oxazolidines is experimentally simple, broad substrate scope, good yields, and excellent regioselectivity.

Язык: Английский

Процитировано

0
Scaffold-Hopping Strategies in Aurone Optimization: A Comprehensive Review of Synthetic Procedures and Biological Activities of Nitrogen and Sulfur Analogues DOI Creative Commons
Gabriele La Monica, Federica Alamia, Alessia Bono

и другие.

Molecules, Год журнала: 2024, Номер 29(12), С. 2813 - 2813

Опубликована: Июнь 13, 2024

Aurones, particular polyphenolic compounds belonging to the class of minor flavonoids and overlooked for a long time, have gained significative attention in medicinal chemistry recent years. Indeed, considering their unique outstanding biological properties, they stand out as an intriguing reservoir new potential lead drug discovery context. Nevertheless, several physicochemical, pharmacokinetic, pharmacodynamic (P3) issues hinder progression more advanced phases pipeline, making optimization campaigns necessary. In this context, scaffold hopping has proven be valuable approach natural products. This review provides comprehensive updated picture scaffold-hopping approaches directed at synthetic aurones. literature analysis, focus is given nitrogen sulfur analogues. For each presented, general procedures are summarized, highlighting key advantages issues. Furthermore, activities most representative scaffold-hopped emphasizing improvements achieved further compared aurone class.

Язык: Английский

Процитировано

2