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Synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities
Author(s) -
Faiza Ahad,
Nida Ghouri,
Khalid Mohammed Khan,
Shahnaz Perveen,
M. Iqbal Choudhary
Publication year - 2018
Publication title -
royal society open science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.84
H-Index - 51
ISSN - 2054-5703
DOI - 10.1098/rsos.171771
Subject(s) - benzophenone , leishmaniasis , sandfly , pentamidine , in vitro , leishmania major , leishmania , amastigote , chemistry , mass spectrometry , stereochemistry , combinatorial chemistry , parasite hosting , biology , organic chemistry , biochemistry , chromatography , immunology , medicine , computer science , world wide web , pneumonia
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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