Synthesis and Structure-Activity Relationships of New Chiral Spiro-β-lactams Highly Active Against HIV-1 and Plasmodium
2021
Abstract The synthesis and anti-microbial 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.
- Correction
- Source
- Cite
- Save
- Machine Reading By IdeaReader
50
References
2
Citations
NaN
KQI