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Discovery of new S-adenosylmethionine decarboxylase inhibitors for the treatment of Human African Trypanosomiasis (HAT).

Drug and Biomaterial R&D, Genzyme Corporation, Waltham, MA 02451, United States.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.65). 07/2009; 19(11):2916-9. DOI: 10.1016/j.bmcl.2009.04.096
Source: PubMed

ABSTRACT Modification of the structure of trypanosomal AdoMetDC inhibitor 1 (MDL73811) resulted in the identification of a new inhibitor 7a, which features a methyl substituent at the 8-position. Compound 7a exhibits improved potencies against both the trypanosomal AdoMetDC enzyme and parasites, and better blood brain barrier penetration than 1.

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