Synthesis, biological evaluation and molecular docking studies of quinoline‐conjugated 1,2,3‐triazole derivatives as antileishmanial agents

In the present work, we have synthesized novel quinoline‐conjugated 1,2,3‐triazole derivatives 6a–l starting from substituted acetanilides in five steps. The synthesized compounds were screened for their antileishmanial activity. Quinoline‐conjugated 1,2,3‐triazole compounds 6c (IC50 = 15.1 μg/ml),...

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Veröffentlicht in:Journal of heterocyclic chemistry 2022-04, Vol.59 (4), p.739-749
Hauptverfasser: Tapkir, Sandeep R., Patil, Rajendra H., Galave, Sharad A., Phadtare, Ganesh R., Khedkar, Vijay M., Garud, Dinesh R.
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Sprache:eng
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Zusammenfassung:In the present work, we have synthesized novel quinoline‐conjugated 1,2,3‐triazole derivatives 6a–l starting from substituted acetanilides in five steps. The synthesized compounds were screened for their antileishmanial activity. Quinoline‐conjugated 1,2,3‐triazole compounds 6c (IC50 = 15.1 μg/ml), 6d (IC50 = 14.6 μg/ml) and 6e (IC50 = 14.3 μg/ml) displayed potent antileishmanial activity when compared with standard sodium stibogluconate (IC50 = 14.3 ± 1.5 μg/ml). A molecular docking study against Leishmania major pteridine reductase (Lm‐PTR1) suggests that these compounds have the potential to become lead molecules in antileishmanial drug discovery. Quinoline‐conjugated 1,2,3‐triazole derivatives as antileishmanial agents
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.4414