Journal of Medicinal Chemistry
BRIEF ARTICLE
’ EXPERIMENTAL SECTION: CHEMISTRY
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General Procedure for the Preparation of the Hydroxamic
Acids 7aꢀe, 8, 9aꢀd, 10a, and 10b. A solution of the appropriate
O-benzyl hydroxamate (1 mmol) in absolute EtOH (40 mL) was
hydrogenated (PdꢀC 10%, 45 mg) for 3 h at room temperature and
50 psi. The catalyst was filtered off, washed with EtOH (3 ꢁ 10 mL), and
the combined filtrates were evaporated in vacuo. Purification of the
residue by column chromatography on silica gel using AcOEtꢀMeOH
5:1 (7a, 7b, 9a) or AcOEt (7cꢀe, 8, 9bꢀd, 10a, 10b) provided the pure
hydroxamic acid as a white crystalline or foamy solid (Supporting
Information).
’ ASSOCIATED CONTENT
S
Supporting Information. Synthesis details of 7aꢀe, 8,
b
9aꢀd, 10a, 10b, 43ꢀ45, 14, 19, 24, 29, 32, 37, 6b, 40, 41, 66, 68,
and 70; chemical and physical data; antitrypanosome action data
of 43ꢀ45, 27ꢀ31, 41, 56, 59, 71, 6a, 6b, 37ꢀ39, and 64ꢀ67;
biological assays; elemental analysis data of the tested com-
pounds. This material is available free of charge via the Internet at
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’ AUTHOR INFORMATION
Corresponding Author
*Phone: þ30210 7274810. Fax: þ30210 7274747. E-mail: gfytas@
pharm.uoa.gr.
’ ACKNOWLEDGMENT
This work was partially supported by a research grant from the
University of Athens, Greece (ELKE Account KA 70/4/7841).
J.M.K. acknowledges the support of the Wellcome Trust (Grant
No. 084175).
’ ABBREVIATIONS USED
2,6-DKP, 2,6-diketopiperazine; MMP, matrix metalloproteinase;
HDAC, histone deacetylase; 5-LO, 5-lipoxygenase; TbPGDH,
T. brucei 6-phosphoglyconate dehydrogenase; 6-PGDH, 6-phos-
phoglyconate dehydrogenase; CDI, 1,10-carbonyldiimidazole;
SI, selectivity index
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