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Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype
Daniel P Brooke1, Leah M C McGee1, Federica Giordani2
1WestCHEM Department of Pure and Applied Chemistry, University of Strathclyde Glasgow UK fraser.j.scott@strath.ac.uk.
RSC Medicinal Chemistry
|August 27, 2021
Summary
Researchers synthesized truncated Strathclyde minor groove binders (S-MGBs) to mimic disgocidine. A lead compound showed selective activity against trypanosomes and Leishmania, with reduced aggregation.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Parasitology
Background:
- Strathclyde minor groove binders (S-MGBs) exhibit broad bioactivity.
- There is a need for selective antiparasitic agents.
- Natural product disgocidine serves as a structural template.
Purpose of the Study:
- To design and synthesize truncated S-MGBs.
- To evaluate the antiparasitic activity of these compounds.
- To investigate the impact of truncation on S-MGB aggregation.
Main Methods:
- Chemical synthesis of seven truncated S-MGB analogues.
- Antiparasitic and antibacterial activity screening.
- 1H NMR and Diffusion Ordered Spectroscopy (DOSY) for aggregation studies.
Main Results:
- A lead truncated S-MGB demonstrated significant activity against trypanosomes and Leishmania.
- Truncation strategy reduced aggregation in aqueous environments compared to full-length S-MGBs.
- Selective activity profile achieved, minimizing broader organismal effects.
Conclusions:
- Truncated S-MGBs represent a promising scaffold for developing novel antiparasitic drugs.
- The lead compound warrants further investigation for treating trypanosomiasis and leishmaniasis.
- Structural modification can mitigate aggregation issues in S-MGBs.
