Bioactive atropisomers: Unraveling design strategies and synthetic routes for drug discovery.
Med Res Rev
; 44(5): 1971-2014, 2024 09.
Article
em En
| MEDLINE
| ID: mdl-38515232
ABSTRACT
Atropisomerism, an expression of axial chirality caused by limited bond rotation, is a prominent aspect within the field of medicinal chemistry. It has been shown that atropisomers of a wide range of compounds, including established FDA-approved drugs and experimental molecules, display markedly different biological activities. The time-dependent reversal of chirality in atropisomers poses complexity and obstacles in the process of drug discovery and development. Nonetheless, recent progress in understanding atropisomerism and enhanced characterization methods have greatly assisted medicinal chemists in the effective development of atropisomeric drug molecules. This article provides a comprehensive review of their special design thoughts, synthetic routes, and biological activities, serving as a reference for the synthesis and biological evaluation of bioactive atropisomers in the future.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
/
Descoberta de Drogas
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Med Res Rev
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
China