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Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni
- Source :
- ACS Medicinal Chemistry Letters
- Publication Year :
- 2020
- Publisher :
- American Chemical Society, 2020.
-
Abstract
- We recently reported a series of compounds for a solubility-driven optimization campaign of antitrypanosomal compounds. Extending a parasite-hopping approach to the series, a subset of compounds from this library has been cross-screened for activity against the metazoan flatworm parasite, Schistosoma mansoni. This study reports the identification and preliminary development of several potently bioactive compounds against adult schistosomes, one or more of which represent promising leads for further assessment and optimization.
- Subjects :
- Flatworm
Parasite-hopping
Letter
biology
010405 organic chemistry
Organic Chemistry
Neglected tropical disease
Schistosomiasis
Computational biology
medicine.disease
Lapatinib
biology.organism_classification
01 natural sciences
Biochemistry
0104 chemical sciences
3. Good health
010404 medicinal & biomolecular chemistry
Schistosoma spp
Drug Discovery
medicine
Parasite hosting
Schistosoma mansoni
Target class repurposing
medicine.drug
Subjects
Details
- Language :
- English
- ISSN :
- 19485875
- Volume :
- 11
- Issue :
- 3
- Database :
- OpenAIRE
- Journal :
- ACS Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....dd8ee50ddcb2576fc6178e843d54b7e1