期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 24, 页码 5907-5910出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.11.006
关键词
Benzimidazole diamidines; DAPI; DNA minor groove binders; Antitrypanosomal activity
资金
- Bill and Melinda Gates Foundation through the Consortium for Parasitic Drug Development
A series of novel benzimidazole diamidines were prepared from the corresponding dicyano analogues either by applying Pinner methodology (5a-c, 10 and 13a) or by making amidoximes intermediates that were reduced to the corresponding amidines (15a-c). The new amidines were evaluated in vitro against the protozoan parasite Trypanosoma brucei rhodesiense (T. b. r.). The thiophene analogue 5b and the N-methyl compound 15a showed superior antitrypanosomal activity compared to that of the parent I. Published by Elsevier Ltd.
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