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Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.

Bioorganic & medicinal chemistry (2009-11-17)
Vishal Patil, William Guerrant, Po C Chen, Berkley Gryder, Derek B Benicewicz, Shabana I Khan, Babu L Tekwani, Adegboyega K Oyelere
ABSTRACT

Histone deacetylase inhibitors (HDACi) are endowed with plethora of biological functions including anti-proliferative, anti-inflammatory, anti-parasitic, and cognition-enhancing activities. Parsing the structure-activity relationship (SAR) for each disease condition is vital for long-term therapeutic applications of HDACi. We report in the present study specific cap group substitution patterns and spacer-group chain lengths that enhance the antimalarial and antileishmanial activity of aryltriazolylhydroxamates-based HDACi. We identified many compounds that are several folds selectively cytotoxic to the plasmodium parasites compared to standard HDACi. Also, a few of these compounds have antileishmanial activity that rivals that of miltefosine, the only currently available oral agent against visceral leishmaniasis. The anti-parasite properties of several of these compounds tracked well with their anti-HDAC activities. The results presented here provide further evidence on the suitability of HDAC inhibition as a viable therapeutic option to curb infections caused by apicomplexan protozoans and trypanosomatids.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
O-Tritylhydroxylamine, 95%

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