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. 2009 Jun 1;19(11):2916-9.
doi: 10.1016/j.bmcl.2009.04.096. Epub 2009 Apr 24.

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

Bradford Hirth  1 , Robert H Barker Jr, Cassandra A Celatka, Jeffrey D Klinger, Hanlan Liu, Bakela Nare, Amarjit Nijjar, Margaret A Phillips, Edmund Sybertz, Erin K Willert, Yibin Xiang
Affiliations

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

Bradford Hirth et al. Bioorg Med Chem Lett. .

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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