Accepting the Invitation to Open Innovation in Malaria Drug Discovery: Synthesis, Biological Evaluation, and Investigation on the Structure–Activity Relationships of Benzo[b]thiophene-2-carboxamides as Antimalarial Agents
| العنوان: | Accepting the Invitation to Open Innovation in Malaria Drug Discovery: Synthesis, Biological Evaluation, and Investigation on the Structure–Activity Relationships of Benzo[b]thiophene-2-carboxamides as Antimalarial Agents |
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| المؤلفون: | Marco Pieroni, Federica Vacondio, Michal Zolkiewski, Gabriele Costantino, Elisa Azzali, Nicoletta Basilico, Silvia Parapini, Giannamaria Annunziato, Claudia Beato, Agostino Bruno |
| المصدر: | Journal of Medicinal Chemistry. 60:1959-1970 |
| بيانات النشر: | American Chemical Society (ACS), 2017. |
| سنة النشر: | 2017 |
| مصطلحات موضوعية: | 0301 basic medicine, Combination therapy, Phenotypic screening, Drug Evaluation, Preclinical, Thiophenes, Pharmacology, Biology, 01 natural sciences, Antimalarials, Structure-Activity Relationship, 03 medical and health sciences, parasitic diseases, Drug Discovery, medicine, Humans, Structure–activity relationship, Antimalarial Agent, Artemisinin, Biological evaluation, 010405 organic chemistry, Drug discovery, medicine.disease, Amides, 0104 chemical sciences, 030104 developmental biology, Molecular Medicine, Malaria, medicine.drug |
| الوصف: | Malaria eradication is a global health priority, but current therapies are not always suitable for providing a radical cure. Artemisinin has paved the way for the current malaria treatment, the so-called Artemisinin-based Combination Therapy (ACT). However, with the detection of resistance to ACT, innovative compounds active against multiple parasite species and at multiple life stages are needed. GlaxoSmithKline has recently disclosed the results of a phenotypic screening of an internal library, publishing a collection of 400 antimalarial chemotypes, termed the "Malaria Box". After analysis of the data set, we have carried out a medicinal chemistry campaign in order to define the structure-activity relationships for one of the released compounds, which embodies a benzothiophene-2-carboxamide core. Thirty-five compounds were prepared, and a description of the structural features responsible for the in vitro activity against different strains of P. falciparum, the toxicity, and the metabolic stability is herein reported. |
| تدمد: | 1520-4804 0022-2623 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f39422e4151f55e69e5ae0eaace5dd4 https://doi.org/10.1021/acs.jmedchem.6b01685 |
| رقم الأكسشن: | edsair.doi.dedup.....7f39422e4151f55e69e5ae0eaace5dd4 |
| قاعدة البيانات: | OpenAIRE |
Find this issue from the American Chemical Society | تدمد: | 15204804 00222623 |
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