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http://hdl.handle.net/1843/41573| Type: | Artigo de Periódico |
| Title: | Synthesis of quinoline derivatives as potential cysteine protease inhibitors |
| Other Titles: | Síntese de derivados de quinolina como potenciais inibidores de protease de cisteína |
| Authors: | Marina M. S. Andrade Rafaela S. Ferreira Renata B. Oliveira Luan Carvalho Martins Gabriel V. Marques Carla A. Silva Gilson Faria Sérgio Caldas Janete S. Dos Santos Sophie Y. Leclercq Vinícius G. Maltarollo |
| Abstract: | Aim: Cysteine proteases are important molecular targets involved in the replication, virulence and survival of parasitic organisms, including Trypanosoma and Leishmania species. Methodology & results: Analogs of the 7-chloro-N-[3-(morpholin-4-yl)propyl]quinolin-4-amine were synthesized and their inhibitory activity against the enzymes cruzain and rhodesain as well as against promastigotes forms of Leishmania species and epimastigotes forms of Trypanosoma cruzi were evaluated. Five compounds showed activity against both enzymes with half maximal inhibitory concentration (IC50) values ranging from 23 to 123 μM. Among these, compounds 3 and 4 displayed leishmanicidal activity; compound 4 was the most promising with IC50 values <10 μM and no cytotoxicity for uninfected cells. Conclusion: The results obtained indicate that cysteine proteases are likely to be the molecular target of compounds 3 and 4. |
| Abstract: | Objetivo: As proteases de cisteína são importantes alvos moleculares envolvidos na replicação, virulência e sobrevivência de organismos parasitários, incluindo espécies de Trypanosoma e Leishmania. Metodologia e resultados: Análogos da 7-cloro-N-[3-(morfolin-4-il)propil]quinolin-4-amina foram sintetizados e sua atividade inibitória contra as enzimas cruzaína e rodesaína, bem como contra as formas promastigotas de Leishmania foram avaliadas espécies e formas epimastigotas de Trypanosoma cruzi. Cinco compostos mostraram atividade contra ambas as enzimas com metade dos valores de concentração inibitória máxima (IC50) variando de 23 a 123 μM. Dentre estes, os compostos 3 e 4 apresentaram atividade leishmanicida; o composto 4 foi o mais promissor com valores de IC50 <10 μM e sem citotoxicidade para células não infectadas. Conclusão: Os resultados obtidos indicam que as proteases de cisteína são provavelmente o alvo molecular dos compostos 3 e 4. |
| Subject: | Atividade antiparasitária 4-Aminoquinolinas Protease de cisteína |
| language: | eng |
| metadata.dc.publisher.country: | Brasil |
| Publisher: | Universidade Federal de Minas Gerais |
| Publisher Initials: | UFMG |
| metadata.dc.publisher.department: | FAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS ICB - DEPARTAMENTO DE BIOQUÍMICA E IMUNOLOGIA ICX - DEPARTAMENTO DE QUÍMICA |
| Rights: | Acesso Restrito |
| metadata.dc.identifier.doi: | 10.4155/fmc-2019-0201 |
| URI: | http://hdl.handle.net/1843/41573 |
| Issue Date: | 2020 |
| metadata.dc.url.externa: | https://www.future-science.com/doi/full/10.4155/fmc-2019-0201 |
| metadata.dc.relation.ispartof: | Future medicinal chemistry |
| Appears in Collections: | Artigo de Periódico |
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