| Author | Rabelo, Vitor Won-Held | |
| Author | Carneiro, Leonardo Simões de Abreu | |
| Author | Martins, Luan Letieri Belem | |
| Author | Souza, Fernando Almeida de | |
| Author | Silva, Luciene Soares | |
| Author | Amorim, Leonardo dos Santos Corrêa | |
| Author | Sanchez Nuñez, Maria Leonisa | |
| Author | Calabrese, Kátia da Silva | |
| Author | Abreu, Paula Alvarez | |
| Author | Müller, Camilla Djenne Buarque | |
| Author | Paixão, Izabel Christina Nunes de Palmer | |
| Access date | 2025-02-17T16:53:22Z | |
| Available date | 2025-02-17T16:53:22Z | |
| Document date | 2024 | |
| Citation | RABELO, Vitor Won-Held et al. Biological evaluation of 3-Aryl and/or 4-(N-Aryl)aminocoumarins against human pathogens: antileishmanial and antiviral activities. Future Pharmacology, v. 4, n. 4, p. 919-933, 19 Dec. 2024. | |
| ISSN | 2673-9879 | |
| URI | https://www.arca.fiocruz.br/handle/icict/68592 | |
| Description | Produção científica do Laboratório de Protozoologia. | pt_BR |
| Sponsorship | This study was financed in part by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior—Brasil (CAPES)—Finance Code 001. In addition, this work was supported by Brazilian agencies including the National Council for Scientific and Technological Development (CNPq) and the Research Support Foundation of the State of Rio de Janeiro (FAPERJ; grant number 26/211.680/2021). Fernando Almeida de Souza is a senior postdoctoral research fellow and scholarship holder of FAPERJ [grant number E-26/203.513/2023] and Katia da Silva Calabrese is a researcher productivity fellow of CNPq [grant number 315225/2021-1]. | |
| Language | eng | en_US |
| Publisher | MDPI | |
| Rights | open access | |
| Title | Biological evaluation of 3-Aryl and/or 4-(N-Aryl)aminocoumarins against human pathogens: antileishmanial and antiviral activities | en_US |
| Type | Article | |
| DOI | 10.3390/futurepharmacol4040048 | |
| Abstract | Background: Vector-borne diseases, such as leishmaniasis and arboviral infections, represent a great challenge to human health with limited therapeutic options. In addition, sexually transmitted infections, such as herpes, affect billions of people worldwide and the emergence of new strains resistant to common antivirals, such as acyclovir (ACV), poses a serious threat to humans. In this context, coumarins have proved to be a valuable source of new derivatives with promising biological activities to fight these diseases. Methodology: 3-aryl and/or 4-(N-aryl)aminocoumarins were synthesized, and their drug-like profile was evaluated using silico tools. Their biological activity against Leishmania amazonensis promastigotes was evaluated using the MTT assay, while their antiviral activity against replication of Chikungunya, Mayaro, Zika, and type 1 Herpes simplex virus (HSV-1) in Vero cells was analyzed using plaque reduction assays. Results: The in silico studies pointed to satisfactory pharmacokinetic and toxicological properties as drug candidates. Hence, their antileishmanial activity was evaluated. None of the compounds exhibited significant activity and compound 2b showed the highest activity (IC50 = 47.10 µM). We further evaluated their cytotoxicity and antiviral activity. Compound 2e showed good activity against ACV-sensitive and -resistant HSV-1 strains with EC50 values of 48.68 µM and 66.26 µM, respectively (selectivity index values of 12.5 and 9.2). Mechanism of action studies indicated that this compound acts at late steps of HSV-1 replication, such as virus egress. Conclusions: Compound 2e possesses a different mechanism of action compared to ACV and presents a promising alternative for the treatment of HSV-1 infections. | en_US |
| Affilliation | Universidade Federal Fluminense. Instituto de Biologia. Departamento de Biologia Celular e Molecular. Programa de Pós-Graduação em Ciências e Biotecnologia. Niterói, RJ, Brasil. | |
| Affilliation | Pontifícia Universidade Católica do Rio de Janeiro. Centro Técnico Científico. Laboratório de Síntese Orgânica. Departamento de Química. Rio de Janeiro, RJ, Brasil / Universidade Federal Rural do Rio de Janeiro. Instituto de Química. Departamento de Química Orgânica. Grupo de Nanotecnologia e Química Orgânica. Seropédica, RJ, Brasil. | |
| Affilliation | Universidade Federal Fluminense. Instituto de Biologia. Departamento de Biologia Celular e Molecular. Programa de Pós-Graduação em Ciências e Biotecnologia. Niterói, RJ, Brasil. | |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Protozoologia. Rio de Janeiro, RJ, Brasil / Universidade Estadual do Maranhão. Centro de Ciências Agrárias. São Luís, MA, Brasil. | |
| Affilliation | Universidade Federal Fluminense. Instituto de Biologia. Departamento de Biologia Celular e Molecular. Programa de Pós-Graduação em Ciências e Biotecnologia. Niterói, RJ, Brasil. | |
| Affilliation | Universidade Federal Fluminense. Instituto de Biologia. Departamento de Biologia Celular e Molecular. Programa de Pós-Graduação em Ciências e Biotecnologia. Niterói, RJ, Brasil / Governo do Estado Rio de Janeiro. Instituto Vital Brazil S.A. Gerência de Desenvolvimento Tecnológico Niterói, RJ, Brasil. | |
| Affilliation | Universidade Federal Fluminense. Instituto de Biologia. Departamento de Biologia Celular e Molecular. Niterói, RJ, Brasil. | |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Protozoologia. Rio de Janeiro, RJ, Brasil. | |
| Affilliation | Universidade Federal do Rio de Janeiro. Centro de Ciências da Saúde. Instituto de Biodiversidade e Sustentabilidade. Macaé, RJ, Brasil. | |
| Affilliation | Pontifícia Universidade Católica do Rio de Janeiro. Centro Técnico Científico. Laboratório de Síntese Orgânica. Departamento de Química. Rio de Janeiro, RJ, Brasil. | |
| Affilliation | Universidade Federal Fluminense. Instituto de Biologia. Departamento de Biologia Celular e Molecular. Niterói, RJ, Brasil. | |
| Subject | Coumarins | en_US |
| Subject | Antileishmanial | en_US |
| Subject | Antiviral | en_US |
| Subject | Arboviruses | en_US |
| Subject | HSV-1 | en_US |
| DeCS | Herpesvirus Humano 1 | pt_BR |
| e-ISSN | 2673-9879 | |
| xmlui.metadata.dc.subject.ods | 03 Saúde e Bem-Estar | |
| xmlui.metadata.dc.subject.ods | 09 Indústria, inovação e infraestrutura | |
