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1.
Bioorg Chem ; 150: 107525, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38852308

RESUMO

This review explores the recent advancements in the design and synthesis of pseudo-natural products (pseudo-NPs) by employing innovative principles and strategies, heralding a transformative era in chemistry and biology. Pseudo-NPs, produced through in silico fragmentation and the de novo recombination of natural product fragments, reveal compounds endowed with distinct biological activities. Their advantage lies in transcending natural product structures, fostering diverse possibilities. Research in this area over the past decade has yielded unconventional combinations of natural product fragments, leading to the identification of novel compounds possessing unique scaffolds and biological significance, thereby contributing to the discovery of new therapeutics. The pseudo-NPs exert potent biological effects through various signaling pathways. In chemical biology and medicinal chemistry, designing pseudo-NPs is an important strategy, harnessing molecular hybridization and bioinspired synthesis to generate diverse compounds with remarkable biological activities, underscoring their immense potential in drug discovery and development.


Assuntos
Produtos Biológicos , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Produtos Biológicos/síntese química , Humanos , Estrutura Molecular , Descoberta de Drogas , Animais
2.
Org Biomol Chem ; 22(26): 5242-5256, 2024 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-38881404

RESUMO

This review explores the significance of trifluoromethylnitrones in synthesizing fluorine-containing compounds, with a particular focus on trifluoromethylated heterocycles. It explores the versatility of trifluoromethylnitrones, especially in [3 + 2] cycloaddition reactions, highlighting their unique reactivity with various dienophile substrates. Trifluoromethylnitrones are valuable precursors for the rapid synthesis of medicinally important trifluoromethylated heterocycles, including isoxazolidines, dihydroisoxazoles, oxathiazolidines, ß-lactams, and aziridines. These heterocycles, in turn, serve as synthons for synthesizing trifluoromethylated lactams and aminoalcohols. Additionally, nitrone chemistry extends to synthesizing trifluoromethylated nucleosides and trifluorinated organoborane heterocycles, demonstrating their versatility. While sharing similarities with trifluorodiazoethane reactivity, trifluoromethylnitrones offer distinct advantages by enabling the synthesis of heterocycles typically inaccessible with trifluorodiazoethane.

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