@article{59960f42b60d4fe7a3b670ab9f9bf915,
title = "Discovery of new S-adenosylmethionine decarboxylase inhibitors for the treatment of Human African Trypanosomiasis (HAT)",
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.",
keywords = "Blood brain barrier, Inhibitor, Purine, S-Adenosylmethionine decarboxylase (AdoMetDC), Sleeping sickness, Trypanosomiasis",
author = "Bradford Hirth and Barker, {Robert H.} and Celatka, {Cassandra A.} and Klinger, {Jeffrey D.} and Hanlan Liu and Bakela Nare and Amarjit Nijjar and Phillips, {Margaret A.} and Edmund Sybertz and Willert, {Erin K.} and Yibin Xiang",
note = "Funding Information: The authors would like to thank Drs. Patrick Casara, Simon Croft, Reto Brun and Robert Don for helpful discussions throughout these studies. This work was supported in part by funding from DNDi and by resources provided by Genzyme. Genzyme is committed to assisting in discovery of drugs for neglected diseases in collaboration with other partners and seeks no profit from drugs used for these applications (Bacchi et al., mss submitted).",
year = "2009",
month = jun,
day = "1",
doi = "10.1016/j.bmcl.2009.04.096",
language = "English (US)",
volume = "19",
pages = "2916--2919",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Ltd",
number = "11",
}