The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Structure-Activity Relationships for Inhibition of Cysteine Protease Activity and Development of Plasmodium falciparum by Peptidyl Vinyl Sulfones
Open accessAbstract
The Plasmodium falciparum cysteine proteases falcipain-2 and falcipain-3 appear to be required for hemoglobin hydrolysis by intraerythrocytic malaria parasites. Previous studies showed that peptidyl vinyl sulfone inhibitors of falcipain-2 blocked the development of P. falciparum in culture and exerted antimalarial effects in vivo. We now report the structure-activity relationships for inhibition of falcipain-2, falcipain-3, and parasite development by 39 new vinyl sulfone, vinyl sulfonate ester, and vinyl sulfonamide cysteine protease inhibitors. Levels of inhibition of falcipain-2 and falcipain-3 were generally similar, and many potent compounds were identified. Optimal antimalarial compounds, which inhibited P. falciparum development at low nanomolar concentrations, were phenyl vinyl sulfones, vinyl sulfonate esters, and vinyl sulfonamides with P 2 leucine moieties. Our results identify independent structural correlates of falcipain inhibition and antiparasitic activity and suggest that peptidyl vinyl sulfones have promise as antimalarial agents.
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Cites
The economic and social burden of malaria
Sachs, J., & Malaney, P. (2002) · Nature · doi:10.1038/415680a · Cited by 2,248 · cited 1×
“Plasmodium falciparum, the most virulent human malaria parasite, is estimated to cause over 300 million new cases and 1 million deaths annually (33).”
BackgroundA malarial cysteine proteinase is necessary for hemoglobin degradation by Plasmodium falciparum
Rosenthal, P. J., McKerrow, J. H., Aikawa, M., Nagasawa, H., & Leech, J. H. (1988) · Journal of Clinical Investigation · doi:10.1172/jci113766 · Cited by 331
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Cited by
A Medicinal Chemistry Perspective on Artemisinin and Related Endoperoxides
O'Neill, P. M., & Posner, G. H. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm030571c · Cited by 538
Metadata
- Authors
- Shenai, B. R., Lee, B. J., Alvarez-Hernandez, A., Chong, P. Y., Emal, C. D., Neitz, R. J., Roush, W. R., & Rosenthal, P. J.
- Venue
- Antimicrobial Agents and Chemotherapy
- Publisher
- American Society for Microbiology
- Published
- 2003-01
- Volume
- 47
- Issue
- 1
- Pages
- 154-160
- ISSN
- 0066-4804 (ISSN-L)
- 1098-6596
- OpenAlex
- W2083762132
- Cited by
- 160
- References
- 2
- FWCI
- 6.00
- Type
- journal article
- Language
- en
- Open access
- green
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- Shenai, B. R., Lee, B. J., Alvarez-Hernandez, A., Chong, P. Y., Emal, C. D., Neitz, R. J., Roush, W. R., & Rosenthal, P. J. (2003). Structure-Activity Relationships for Inhibition of Cysteine Protease Activity and Development of Plasmodium falciparum by Peptidyl Vinyl Sulfones. Antimicrobial Agents and Chemotherapy. https://doi.org/10.1128/aac.47.1.154-160.2003
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
