发现用于治疗人类非洲锥虫病（HAT）的新型S-腺苷甲硫氨酸脱羧酶抑制剂。
Discovery of new S-adenosylmethionine decarboxylase inhibitors for the treatment of Human African Trypanosomiasis (HAT).
作者信息
Hirth Bradford, Barker Robert H, Celatka Cassandra A, Klinger Jeffrey D, Liu Hanlan, Nare Bakela, Nijjar Amarjit, Phillips Margaret A, Sybertz Edmund, Willert Erin K, Xiang Yibin
机构信息
Drug and Biomaterial R&D, Genzyme Corporation, Waltham, MA 02451, United States.
出版信息
Bioorg Med Chem Lett. 2009 Jun 1;19(11):2916-9. doi: 10.1016/j.bmcl.2009.04.096. Epub 2009 Apr 24.
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.
对锥虫腺苷甲硫氨酸脱羧酶抑制剂1（MDL73811）的结构进行修饰后，鉴定出一种新的抑制剂7a，其在8位具有一个甲基取代基。化合物7a对锥虫腺苷甲硫氨酸脱羧酶和寄生虫均表现出更高的效力，并且比1具有更好的血脑屏障穿透性。
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