Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes

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Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes

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作者：Avninder S. Bhambra^a ; ^{abhambra@dmu.ac.uk" class="auth_mail" title="E-mail the corresponding author} ; Mark Edgar^b ; Mark R.J. Elsegood^b ; ^{m.r.j.elsegood@lboro.ac.uk" class="auth_mail" title="E-mail the corresponding author} ; Yuqi Li^b ; George W. Weaver^b ; ^{g.w.weaver@lboro.ac.uk" class="auth_mail" title="E-mail the corresponding author} ; Randolph R.J. Arroo^c ; Vanessa Yardley^d ; Hollie Burrell-Saward^d ; Vladimir Krystof^e
关键词：Benzothiophenes ; Fluorinated drugs ; Antitrypanosomal activity ; Sleeping sickness ; Human African Trypanosomiasis ; Trypanosoma brucei rhodesiense
刊名：European Journal of Medicinal Chemistry
出版年：2016
出版时间：27 January 2016
年：2016
卷：108
期：Complete
页码：347-353
全文大小：623 K

文摘

•: Perfluorinated building blocks used in synthesis of heterocyclic scaffolds.
•: S_NAr substitution reactions employed to deliver 6-benzimidazol-1-ylbenzothiophenes.
•: IC₅₀ values of lead compounds were <1 μM against Trypanosoma brucei rhodesiense.

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