Assessing different thiazolidine and thiazole based compounds as antileishmanial scaffolds
| Autor: | Petr Džubák, Roman Lesyk, Marian Hajduch, Pavel G. Polishchuk, Anna Kryshchyshyn-Dylevych, Serhiy Holota, Ermin Schadich, Sona Gurska |
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| Rok vydání: | 2020 |
| Předmět: |
Stereochemistry
Trypanosoma brucei gambiense Clinical Biochemistry Thiazolidine Trypanosoma brucei brucei Pharmaceutical Science 01 natural sciences Biochemistry Small Molecule Libraries chemistry.chemical_compound Structure-Activity Relationship Parasitic Sensitivity Tests Drug Discovery Humans Leishmania major Thiazole Molecular Biology IC50 Primary (chemistry) biology Molecular Structure 010405 organic chemistry Organic Chemistry Fibroblasts biology.organism_classification Trypanocidal Agents In vitro 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry Molecular Medicine Thiazolidines |
| Zdroj: | Bioorganicmedicinal chemistry letters. 30(23) |
| ISSN: | 1464-3405 |
| Popis: | The compounds from eight different thiazolidine and thiazole series were assessed as potential antileishmanial scaffolds. They were tested for antileishmanial activity against promastigotes of Leishmania major using in vitro primary screen and dose response assays. The compounds from six thiazolidine and thiazole series were identified as the hits with antileishmanial activity against L. major. However, the analyses of structure-activity relations (SARs) showed that the interpretable SARs were obtained only for phenyl-indole hybrids (compounds C1, C2, C3 and C5) as the most effective compounds against L. major promastigotes (IC50 |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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