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

…, CA Celatka, JD Klinger, H Liu, B Nare, A Nijjar…

文献索引：Hirth, Bradford; Barker Jr., Robert H.; Celatka, Cassandra A.; Klinger, Jeffrey D.; Liu, Hanlan; Nare, Bakela; Nijjar, Amarjit; Phillips, Margaret A.; Sybertz, Edmund; Willert, Erin K.; Xiang, Yibin Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 11 p. 2916 - 2919

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被引用次数: 17

摘要

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.