Anti-Leishmanial and Cytotoxic Activities of a Series of Maleimides: Synthesis, Biological Evaluation and Structure-Activity Relationship

In the present study, 45 maleimides have been synthesized and evaluated for anti-leishmanial activities against 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-leishmania...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2018-11, Vol.23 (11), p.2878
Main Authors: Fan, Yongxian, Lu, Yuele, Chen, Xiaolong, Tekwani, Babu, Li, Xing-Cong, Shen, Yinchu
Format: Article
Language:English
Subjects:
Amphotericin B
anti-leishmanial activity
Antimicrobial agents
Biological activity
Cytotoxicity
Drug development
Enzymes
Hydrocarbons
In vitro methods and tests
Investigations
Leishmania donovani
maleimides
Parasitic diseases
Pentamidine
SAR
Substitutes
Tropical diseases
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Summary:In the present study, 45 maleimides have been synthesized and evaluated for anti-leishmanial activities against 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 (IC < 0.0128 μg/mL) and (IC < 0.0128 μg/mL), which showed extraordinary efficacy in an in vitro test and low cytotoxicities (CC > 10 μg/mL). The anti-leishmanial activities of and were 10 times better than that of amphotericin B. The structure and activity relationship (SAR) studies revealed that 3,4-non-substituted maleimides displayed the strongest anti-leishmanial activities compared to those for 3-methyl-maleimides and 3,4-dichloro-maleimides. 3,4-dichloro-maleimides were the least cytotoxic compared to 3-methyl-maleimides and 3,4-non-substituted maleimides. The results show that several of the reported compounds are promising leads for potential anti-leishmanial drug development.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules23112878