| Full text | |
| Author(s): |
Dobrachinski, Leandro
;
Ferreira, Leonardo L. G.
;
Cirino, Maria E.
;
Andrade-de-Siqueira, Allan, I
;
Mafud, Ana C.
;
Mascarenhas, Yvonne P.
;
Andricopulo, Adriano D.
;
de Moraes, Josue
Total Authors: 8
|
| Document type: | Journal article |
| Source: | Future Medicinal Chemistry; v. 16, n. 17, p. 9-pg., 2024-07-25. |
| Abstract | |
Aim: To identify potential antischistosomal agents through 3D pharmacophore-based virtual screening of US FDA approved drugs. Materials & methods: A comprehensive virtual screening was conducted on a dataset of 10,000 FDA approved drugs, employing praziquantel as a template. Promising candidates were selected and assessed for their impact on Schistosoma mansoni viability in vitro and in vivo using S. mansoni infected mice. Results & conclusion: Among the selected drugs, betamethasone and doxazosin demonstrated in vitro efficacy, with effective concentration 50% (EC50) values ranging from 35 to 60 mu M. In vivo studies revealed significant (>50%) reductions in worm burden for both drugs. These findings suggest that betamethasone and doxazosin hold promise for repurposing in treating schistosomiasis. Additionally, the study showcases a useful approach for identifying new antischistosomal drugs. (AU) | |
| FAPESP's process: | 16/18023-5 - Preclinical studies with epiisopiloturine and epiisopilosine and their effect against other helminths |
| Grantee: | Ana Carolina Mafud |
| Support Opportunities: | Scholarships abroad - Research Internship - Post-doctor |
| FAPESP's process: | 14/02282-6 - Structure-activity relationship studies about of Pilocarpus microphyllus (Rutaceae) alkaloid derivatives against Schistosoma mansoni |
| Grantee: | Ana Carolina Mafud |
| Support Opportunities: | Scholarships in Brazil - Post-Doctoral |
| FAPESP's process: | 13/25658-9 - Design and Development of Drug Candidates for Chagas Disease |
| Grantee: | Leonardo Luiz Gomes Ferreira |
| Support Opportunities: | Scholarships in Brazil - Post-Doctoral |
| FAPESP's process: | 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery |
| Grantee: | Glaucius Oliva |
| Support Opportunities: | Research Grants - Research, Innovation and Dissemination Centers - RIDC |
| FAPESP's process: | 16/22488-3 - Drug repositioning for neglected diseases: identification of novel anthelmintic agents |
| Grantee: | Josué de Moraes |
| Support Opportunities: | Regular Research Grants |