Journal article
A new chemotype with promise against Trypanosoma cruzi.
- Wang X College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, United States.
- Cal M Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
- Kaiser M Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
- Buckner FS Department of Medicine, University of Washington, 750 Republican Street, Seattle, WA, United States.
- Lepesheva GI Department of Biochemistry, Vanderbilt University, 2200 Pierce Ave., Nashville, TN, United States.
- Sanford AG Department of Biology, University of Nebraska at Omaha, Omaha, NE, United States.
- Wallick AI Department of Biology, University of Nebraska at Omaha, Omaha, NE, United States.
- Davis PH Department of Biology, University of Nebraska at Omaha, Omaha, NE, United States.
- Vennerstrom JL College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, United States. Electronic address: jvenners@unmc.edu.
- 2019-11-11
Published in:
- Bioorganic & medicinal chemistry letters. - 2020
English
Pyridyl benzamide 2 is a potent inhibitor of Trypanosoma cruzi, but not other protozoan parasites, and had a selectivity-index of ≥10. The initial structure-activity relationship (SAR) indicates that benzamide and sulfonamide functional groups, and N-methylpiperazine and sterically unhindered 3-pyridyl substructures are required for high activity against T. cruzi. Compound 2 and its active analogs had low to moderate metabolic stabilities in human and mouse liver microsomes.
- Language
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- English
- Open access status
- closed
- Identifiers
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- DOI 10.1016/j.bmcl.2019.126778
- PMID 31706668
- Persistent URL
- https://sonar.ch/global/documents/247019
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