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.
Original language | English |
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Article number | 113439 |
Journal | European Journal of Medicinal Chemistry |
Volume | 219 |
DOIs | |
Publication status | Published - 5 Jul 2021 |
Keywords
- 1,3-Dipolar Cycloaddition
- 2-butynoates
- Allenes
- Anti-HIV Agents
- Antiplasmodial Agents
- Phosphane-catalyzed [3+2] annulations
- Spiro-3H-pyrazole-β-lactam
- Spiro-penicillanates
- Spirocyclic compounds
- spirocyclopentenyl-β-lactams
- β-Lactams