Synthesis of new praziquantel analogues: Potential candidates for the treatment of schistosomiasis
| Autor: | Singam Naveen Kumar, Malapaka Chandrasekharam, Vaidya Jayathirtha Rao, Partha Sarathi Sadhu, Donato Cioli, Livia Pica-Mattoccia |
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| Rok vydání: | 2012 |
| Předmět: |
Drug
Stereochemistry media_common.quotation_subject Clinical Biochemistry Pharmaceutical Science Schistosomiasis Moderate activity Biochemistry Praziquantel Schistosomicides Structure-Activity Relationship chemistry.chemical_compound Amide parasitic diseases Drug Discovery medicine Animals Molecular Biology media_common Dose-Response Relationship Drug Molecular Structure biology Tetrahydroisoquinoline Organic Chemistry Stereoisomerism Schistosoma mansoni medicine.disease biology.organism_classification Piperazine chemistry Drug Design Molecular Medicine medicine.drug |
| Zdroj: | Bioorganic & medicinal chemistry letters 22 (2012): 1103–1106. doi:10.1016/j.bmcl.2011.11.108 info:cnr-pdr/source/autori:Partha Sarathi Sadhu a; Singam Naveen Kumar a; Malapaka Chandrasekharam b; Livia Pica-Mattoccia c; Donato Cioli c; Vaidya Jayathirtha Rao a/titolo:Synthesis of new Praziquantel analogues: Potential candidates for the treatment of schistosomiasis/doi:10.1016%2Fj.bmcl.2011.11.108/rivista:Bioorganic & medicinal chemistry letters (Print)/anno:2012/pagina_da:1103/pagina_a:1106/intervallo_pagine:1103–1106/volume:22 |
| ISSN: | 0960-894X |
| Popis: | An efficient synthesis of antischistosomal drug praziquantel and analogues was achieved and the synthetic route designed was to afford structurally diverse analogues for better structure–activity relationship understanding. Total of nineteen PZQ analogues with structural variations at amide, piperazine and aromatic moieties have been synthesized and fully characterized. Among all the new analogues tested for antischistosomal activity, one dimethoxy tetrahydroisoquinoline analogue and two tetrahydro-β-carboline analogues exhibited moderate activity against adult Schistosoma mansoni. Tetrahydro-β-carboline analogues showed moderate activity whereas the presence of p-trifluoromethylbenzoyl and p-toluenesulphonyl moieties resulted in complete suppression of antischistosomal activity. |
| Databáze: | OpenAIRE |
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