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Recent advances in synthesis and medicinal chemistry of pyrrolodiazepines
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DOI：10.3389/fchem.2026.1893737.png)
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Abstract
En 中文
Nitrogen-containing heterocyclic compounds represent fundamental structural elements in contemporary medicinal chemistry. Pyrrolodiazepines; which result from the fusion of pyrrole and diazepine rings; integrate the beneficial properties of both parent structures and have emerged as a significant area of research in synthetic chemistry and pharmaceutical development in recent years. This review provides a systematic overview of the synthetic methodologies for pyrrolodiazepine derivatives that have been developed recently; encompassing transition-metal catalysis; cascade cyclization; multicomponent reactions; photoredox catalysis; base-mediated cyclization; and environmentally friendly synthesis approaches. The advantages and limitations of each method are critically evaluated. Furthermore; the biological activities of pyrrolodiazepines are extensively reviewed; addressing their antitumor; antibacterial; antiviral; central nervous system regulatory; metabolic; and cardiovascular effects; along with corresponding structure–activity relationship analyses. Finally; the review identifies the current challenges in the synthesis and application of pyrrolodiazepines and explores potential future development directions.
Keywords:
drug discovery
synthesis
biological activity
heterocyclic chemistry
pyrrolodiazepines
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4.2
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8.3K
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3.2W
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