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Synthesis and Leishmanicidal Activity of 1-[5-(5-Nitrofuran-2-yl)-1, 3, 4-Thiadiazole-2-yl]-4-BenzoylePiperazines

A series of (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a–6e have been synthesized and screened for in-vitro anti-leishmanial activity against the promastigote form of L. major. The structure of Schiff bases were confirmed by (1)H NMR, IR. Screening results indicate that all of the des...

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Detalles Bibliográficos
Autores principales: Foroumadi, Alireza, Adibi, Hadi, Kabudanian Ardestani, Sussan, Shirooie, Samira, Bozorgomid, Arezoo, Jafari, Ali
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5610746/
https://www.ncbi.nlm.nih.gov/pubmed/29201081
Descripción
Sumario:A series of (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a–6e have been synthesized and screened for in-vitro anti-leishmanial activity against the promastigote form of L. major. The structure of Schiff bases were confirmed by (1)H NMR, IR. Screening results indicate that all of the designed and synthesized final compounds (6a-6e) significantly reduced the viability of promastigotes of L. major in comparison toglucantime (IC(50) 3× 10(3) μg/mL). Meta and Para substitutions in benzene ring containing compounds were more potent than other derivative and the most potent compounds were 6d, 6e with IC(50 )value 94 µm and 77.6 µm, respectively. The experimental data proposes that (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives may be further investigated as a candidate drug for treatment of cutaneous leishmaniasis.