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Updated: Nov 8, 2025

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Published on: May 9, 2025
Synthesis and structure-activity relationships of new chiral spiro-β-lactams highly active against HIV-1 and
Nuno Guerreiro Alves1, Inês Bártolo2, Américo J S Alves1
1University of Coimbra, Coimbra Chemistry Centre and Department of Chemistry, 3004-535, Coimbra, Portugal.
Abstract:
The synthesis and antimicrobial activity of new spiro-β-lactams is reported. The design of the new molecules was based on the structural modulation of two previously identified lead spiro-penicillanates with dual activity against HIV and Plasmodium. The spiro-β-lactams synthesized were assayed for their in vitro activity against HIV-1, providing relevant structure-activity relationship information. Among the tested compounds, two spirocyclopentenyl-β-lactams were identified as having remarkable nanomolar activity against HIV-1. Additionally, the same molecules showed promising antiplasmodial activity, inhibiting both the hepatic and blood stages of Plasmodium infection.
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