Abstract
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 IC50 values in the range of 1.19–82.30 µg ml−1, and the values were compared with those of the standard pentamidine (IC50 = 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 1H and 13C nuclear magnetic resonance, electron impact and high-resolution electron impact mass spectrometry and IR.
Highlights
Benzophenone nucleus is found in the aerial part of Gentiana verna L [1] and Garcinia cochinchinensis [2]
Leishmaniasis is initiated when parasite is transmitted to human at metacyclic-flagellated promastigote form
In the light of a previous report on antileishmanial activities of benzophenone ethers [24], structure of pentamidine which possesses ether functionality, and in continuation of our search for antileishmanial agents [25,26,27], we have synthesized a library of functionalized benzophenone ethers and evaluated their antileishmanial activities in vitro
Summary
Benzophenone nucleus is found in the aerial part of Gentiana verna L [1] and Garcinia cochinchinensis [2]. Leishmaniasis is responsible for a high mortality rate worldwide [18,19]. It is a vector-borne protozoan disease, mainly originated from the bite of sandfly. In the light of a previous report on antileishmanial activities of benzophenone ethers [24], structure of pentamidine which possesses ether functionality (figure 1), and in continuation of our search for antileishmanial agents [25,26,27], we have synthesized a library of functionalized benzophenone ethers and evaluated their antileishmanial activities in vitro.
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