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Synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities

Leishmaniasis is a vector-borne protozoan disease; it mainly originates from the bite of sandfly and initiated when parasite is transmitted to human at metacyclic flagellated promastigote form. In the current study, a synthesis of a series of 4-substituted benzophenone ethers 1–20 was carried out in...

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Autores principales: Ahad, Faiza, Ghouri, Nida, Khan, Khalid Mohammed, Perveen, Shahnaz, Choudhary, M. Iqbal
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society Publishing 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5990808/
https://www.ncbi.nlm.nih.gov/pubmed/29892370
http://dx.doi.org/10.1098/rsos.171771
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author Ahad, Faiza
Ghouri, Nida
Khan, Khalid Mohammed
Perveen, Shahnaz
Choudhary, M. Iqbal
author_facet Ahad, Faiza
Ghouri, Nida
Khan, Khalid Mohammed
Perveen, Shahnaz
Choudhary, M. Iqbal
collection PubMed
description Leishmaniasis is a vector-borne protozoan disease; it mainly originates from the bite of sandfly and initiated when parasite is transmitted to human at metacyclic flagellated promastigote form. In the current study, a synthesis of a series of 4-substituted benzophenone ethers 1–20 was carried out in good yields and their in vitro antileishmanial activities were also screened. Among synthetic derivatives, 15 compounds 1, 3, 5–12, 15 and 17–20 showed antileishmanial activities against promastigotes of Leishmania major with IC(50) values in the range of 1.19–82.30 µg ml(−1), and the values were compared with those of the standard pentamidine (IC(50 )= 5.09 ± 0.09 µg ml(−1)). Our study identified a series of new antileishmanial molecules as potential leads. Structures of these synthetic compounds were deduced by different spectroscopic techniques, such as (1)H and (13)C nuclear magnetic resonance, electron impact and high-resolution electron impact mass spectrometry and IR.
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spelling pubmed-59908082018-06-11 Synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities Ahad, Faiza Ghouri, Nida Khan, Khalid Mohammed Perveen, Shahnaz Choudhary, M. Iqbal R Soc Open Sci Chemistry Leishmaniasis is a vector-borne protozoan disease; it mainly originates from the bite of sandfly and initiated when parasite is transmitted to human at metacyclic flagellated promastigote form. In the current study, a synthesis of a series of 4-substituted benzophenone ethers 1–20 was carried out in good yields and their in vitro antileishmanial activities were also screened. Among synthetic derivatives, 15 compounds 1, 3, 5–12, 15 and 17–20 showed antileishmanial activities against promastigotes of Leishmania major with IC(50) values in the range of 1.19–82.30 µg ml(−1), and the values were compared with those of the standard pentamidine (IC(50 )= 5.09 ± 0.09 µg ml(−1)). Our study identified a series of new antileishmanial molecules as potential leads. Structures of these synthetic compounds were deduced by different spectroscopic techniques, such as (1)H and (13)C nuclear magnetic resonance, electron impact and high-resolution electron impact mass spectrometry and IR. The Royal Society Publishing 2018-05-16 /pmc/articles/PMC5990808/ /pubmed/29892370 http://dx.doi.org/10.1098/rsos.171771 Text en © 2018 The Authors. http://creativecommons.org/licenses/by/4.0/ Published by the Royal Society under the terms of the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/, which permits unrestricted use, provided the original author and source are credited.
spellingShingle Chemistry
Ahad, Faiza
Ghouri, Nida
Khan, Khalid Mohammed
Perveen, Shahnaz
Choudhary, M. Iqbal
Synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities
title Synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities
title_full Synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities
title_fullStr Synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities
title_full_unstemmed Synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities
title_short Synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities
title_sort synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5990808/
https://www.ncbi.nlm.nih.gov/pubmed/29892370
http://dx.doi.org/10.1098/rsos.171771
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