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Discovery of new S-adenosylmethionine decarboxylase inhibitors for the treatment of Human African Trypanosomiasis (HAT) |
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| Authors: | Bradford Hirth Robert H Barker Cassandra A Celatka Jeffrey D Klinger Hanlan Liu Bakela Nare Amarjit Nijjar Margaret A Phillips Edmund Sybertz Erin K Willert Yibin Xiang |
| Institution: | 1. Drug and Biomaterial R&D, Genzyme Corporation, 153 Second Avenue, Waltham, MA 02451, United States;2. SCYNEXIS, Inc., 3501C Tricenter Boulevard, Durham, NC 27713, United States;3. University of Texas Southwestern Medical Center, Department of Pharmacology, 6001 Forest Park Road, Dallas, TX 75390-9041, United States |
| 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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