Novel antileishmanial chalconoids: synthesis and biological activity of 1- or 3-(6-chloro-2H-chromen-3-yl)propen-1-ones.
A series of novel chalconoids containing a 6-chloro-2H-chromen-3-yl group were prepared through a convenient and efficient synthetic method by using 5-chloro-2-hydroxybenzaldehyde as starting material. The target compounds were evaluated against the promastigote form of Leishmania major using MTT assay. All of the evaluated compounds have shown high in vitro antileishmanial activity at concentrations less than 3.0 microM. The results of cytotoxicity assessment against mouse peritoneal macrophage cells showed that these compounds display antileishmanial activity at non-cytotoxic concentrations.
Nazarian
Zohreh
Z
Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran.
Emami
Saeed
S
Heydari
Samaneh
S
Ardestani
Sussan K
SK
Nakhjiri
Maryam
M
Poorrajab
Fatemeh
F
Shafiee
Abbas
A
Foroumadi
Alireza
A
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002478:Cells, Cultured; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018320:Leishmania major / Q000187:drug effects*; D017737:Macrophages, Peritoneal / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D013055:Spectrophotometry, Infrared
D000981:Antiprotozoal Agents; D047188:Chalcones