1208863-15-3Relevant articles and documents
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group
Patil, Vishal,Guerrant, William,Chen, Po C.,Gryder, Berkley,Benicewicz, Derek B.,Khan, Shabana I.,Tekwani, Babu L.,Oyelere, Adegboyega K.
experimental part, p. 415 - 425 (2010/03/30)
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.
