2018
DOI: 10.3390/molecules23112878
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Anti-Leishmanial and Cytotoxic Activities of a Series of Maleimides: Synthesis, Biological Evaluation and Structure-Activity Relationship

Abstract: In the present study, 45 maleimides have been synthesized and evaluated for anti-leishmanial activities against L. donovani in vitro and cytotoxicity toward THP1 cells. All compounds exhibited obvious anti-leishmanial activities. Among the tested compounds, there were 10 maleimides with superior anti-leishmanial activities to standard drug amphotericin B, and 32 maleimides with superior anti-leishmanial activities to standard drug pentamidine, especially compounds 16 (IC50 < 0.0128 μg/mL) and 42 (IC50 < 0.0128… Show more

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Cited by 28 publications
(13 citation statements)
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“…The IC 50 values for GEN and CHY were calculated to be 9.9 µg/mL and 13 µg/mL respectively. However, the IC 50 values of evaluated compounds were higher when compared to the IC 50 values of standard drugs like miltefosine (5.42 µg/mL) 50 and amphotericin B (0.12 µg/mL) 51 . The standard drugs like miltefosine and amphotericin B show several side-effects and also drug resistance which makes them inappropriate for the treatment of leishmaniasis but the natural compounds used in our study are non-toxic in nature and also approved by FDA 52,53 .…”
Section: Discussionmentioning
confidence: 79%
“…The IC 50 values for GEN and CHY were calculated to be 9.9 µg/mL and 13 µg/mL respectively. However, the IC 50 values of evaluated compounds were higher when compared to the IC 50 values of standard drugs like miltefosine (5.42 µg/mL) 50 and amphotericin B (0.12 µg/mL) 51 . The standard drugs like miltefosine and amphotericin B show several side-effects and also drug resistance which makes them inappropriate for the treatment of leishmaniasis but the natural compounds used in our study are non-toxic in nature and also approved by FDA 52,53 .…”
Section: Discussionmentioning
confidence: 79%
“…Maleimide is a promising framework because its derivatives have remarkable physical and biological properties (Scheme a). Furthermore, asymmetric Michael addition of maleimides has been extensively investigated because maleimides act as suitable Michael acceptors .…”
mentioning
confidence: 99%
“…The maleimide compound contains a complete imide ring, a structure that exhibits hydrophobicity, allowing it to easily cross cell membranes. And this structure gives the maleimide compound biological activity and medicinal use [ 33 ]. Therefore, we investigated whether maleimide compounds could be developed as novel antifungal agents.…”
Section: Discussionmentioning
confidence: 99%