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…
Index: 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
Full Text: HTML
Citation Number: 17
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.
Related Articles:
Some Synthetic Analogs of the Natural Purine Nucleosides1
[Davoll; Lowy Journal of the American Chemical Society, 1952 , vol. 74, p. 1563,1565]
[Zady, Mona F.; Wong, John L. Journal of Organic Chemistry, 1980 , vol. 45, # 12 p. 2373 - 2377]