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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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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
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author Foroumadi, Alireza
Adibi, Hadi
Kabudanian Ardestani, Sussan
Shirooie, Samira
Bozorgomid, Arezoo
Jafari, Ali
author_facet Foroumadi, Alireza
Adibi, Hadi
Kabudanian Ardestani, Sussan
Shirooie, Samira
Bozorgomid, Arezoo
Jafari, Ali
author_sort Foroumadi, Alireza
collection PubMed
description 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.
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spelling pubmed-56107462017-12-01 Synthesis and Leishmanicidal Activity of 1-[5-(5-Nitrofuran-2-yl)-1, 3, 4-Thiadiazole-2-yl]-4-BenzoylePiperazines Foroumadi, Alireza Adibi, Hadi Kabudanian Ardestani, Sussan Shirooie, Samira Bozorgomid, Arezoo Jafari, Ali Iran J Pharm Res Original Article 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. Shaheed Beheshti University of Medical Sciences 2017 /pmc/articles/PMC5610746/ /pubmed/29201081 Text en © 2017 by School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Foroumadi, Alireza
Adibi, Hadi
Kabudanian Ardestani, Sussan
Shirooie, Samira
Bozorgomid, Arezoo
Jafari, Ali
Synthesis and Leishmanicidal Activity of 1-[5-(5-Nitrofuran-2-yl)-1, 3, 4-Thiadiazole-2-yl]-4-BenzoylePiperazines
title Synthesis and Leishmanicidal Activity of 1-[5-(5-Nitrofuran-2-yl)-1, 3, 4-Thiadiazole-2-yl]-4-BenzoylePiperazines
title_full Synthesis and Leishmanicidal Activity of 1-[5-(5-Nitrofuran-2-yl)-1, 3, 4-Thiadiazole-2-yl]-4-BenzoylePiperazines
title_fullStr Synthesis and Leishmanicidal Activity of 1-[5-(5-Nitrofuran-2-yl)-1, 3, 4-Thiadiazole-2-yl]-4-BenzoylePiperazines
title_full_unstemmed Synthesis and Leishmanicidal Activity of 1-[5-(5-Nitrofuran-2-yl)-1, 3, 4-Thiadiazole-2-yl]-4-BenzoylePiperazines
title_short Synthesis and Leishmanicidal Activity of 1-[5-(5-Nitrofuran-2-yl)-1, 3, 4-Thiadiazole-2-yl]-4-BenzoylePiperazines
title_sort synthesis and leishmanicidal activity of 1-[5-(5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl]-4-benzoylepiperazines
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5610746/
https://www.ncbi.nlm.nih.gov/pubmed/29201081
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