Synthesis and biological evaluation of chalcones as potential antileishmanial agents

Eur J Med Chem. 2014 Jun 23:81:359-66. doi: 10.1016/j.ejmech.2014.05.034.

Shweta Gupta ¹, Rahul Shivahare ², Venkateswarlu Korthikunta ¹, Rohit Singh ¹, Suman Gupta ², Narender Tadigoppula ³

Affiliations

1 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
2 Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
3 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India. Electronic address: t_narendra@cdri.res.in.

PMID: 24858541 DOI: 10.1016/j.ejmech.2014.05.034

Abstract

Antileishmanial activities of thirty-five synthetic Chalcones have been examined. Among them, ten compounds (4, 6, 16, 22, 23, 24, 25, 29, 35 and 37) exhibited potent in vitro activity (IC50 range from 1.70 to 8 μM) against extracellular promastigotes and intracellular amastigotes form of Leishmania donovani. Two promising compounds 22 and 37 were tested in vivo in L. donovani/hamster model. Chalcone 37 showed 83.32% Parasite inhibition at a dose of 50 mg/kg for 10 days whereas, 75.89% Parasite inhibition at 100 mg/kg dose for 5 days by intraperitoneal route at day 7 post-treatment.

Keywords

Antileishmanial; Chromenochalcones; Chromenodihydrochalcones; Leishmania donovani/hamster model.

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