原创力文档discovery of n-(2-aminoethyl)-n-benzyloxyphenyl benzamides new potent trypanosoma brucei inhibitors：（发现n -(2-aminoethyl)-n-benzyloxyphenyl苯甲酰胺新的强有力的锥虫属brucei抑制剂）.pdfVIP
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discovery of n-(2-aminoethyl)-n-benzyloxyphenyl benzamides new potent trypanosoma brucei inhibitors：（发现n -(2-aminoethyl)-n-benzyloxyphenyl苯甲酰胺新的强有力的锥虫属brucei抑制剂）
Bioorganic Medicinal Chemistry 25 (2017) 1571–1584
Contents lists available at ScienceDirect
Bioorganic Medicinal Chemistry
journal homepage: www.el /locate/bmc
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New
potent Trypanosoma brucei inhibitors
Andriy Buchynskyy a, J. Robert Gillespie b, Matthew A. Hulverson b, Joshua McQueen a, Sharon A. Creason b,
Ranae M. Ranade b, Nicole A. Duster b, Michael H. Gelb a,⇑, Frederick S. Buckner b,⇑
a Department of Chemistry, University of Washington, Seattle, WA 98195, USA
b Department of Medicine, University of Washington, Seattle, WA 98109, USA
a r t i c l e i n f o a b s t r a c t
Article history: A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative
Received 8 August 2016 agent of Human African Trypanosomiasis (HAT), led to the identification of N-(2-aminoethyl)-N-phenyl
Revised 9 November 2016 benzamides as a starting point for hit-to-lead medicinal chemistry. Eighty two analogues were prepared,
Accepted 11 November 2016
which led to the identification of a set of highly potent N-(2-aminoethyl)-N-benzyloxyphenyl benzamides
Available online 12 November 2016
with the most potent compound 73 having an in vitro EC50 = 0.001 lM. The compounds displayed drug-
like properties when tested in a number of in vitro assays. Compound 73 was orally bioavailable and dis-
Keywords:
played good pl
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