Design, synthesis and evaluation of novel phenanthridine triazole analogs as potential antileishmanial agents
FUTURE MEDICINAL CHEMISTRY(2022)
Abstract
Aim: To synthesize and screen phenanthridine and 1,2,3-triazole derivatives for antileishmanial activity. Methodology: Synthesized analogs were tested for antileishmanial activity against transgenic strain of Leishmania infantum promastigotes and ex vivo infections. Results: Compounds T01, T08 and T11 revealed significant activity with EC50 T01 with EC50 3.07 mu m is four-fold more potent than the drug miltefosine (EC50 12.6 mu M) against L. infantum promastigotes. In silico studies indicate that the analogs are nontoxic. A molecular docking analysis was also carried out on the T01 and T08 to investigate the binding pattern at the active site of the chosen target trypanothione reductase. Conclusion: The results of this study reveal that phenanthridine triazoles exhibit antileishmanial activity.
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Key words
in silico ADMET prediction, Leishmania infantum, molecular docking, phenanthridine, triazole
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