Abstract：
:Amino acid 1092 (AA1092) in capsid protein 1 of coxsackievirus B3 (CVB3) is located in close vicinity to the central phenoxy group of capsid binders (i.e. pleconaril). Whereas isoleucine is associated with drug susceptibility, leucine and methionine confer resistance to pleconaril. In the present study, novel analogues with different substitutions in the central phenoxy group were synthesized to study their influence on anti-CVB3 activity with the aim to overcome pleconaril resistance. Two [(biphenyloxy)propyl]isoxazoles and pleconaril were synthesized without methyl groups in the central phenoxy ring using Suzuki coupling reaction and tested for antiviral activity against the pleconaril-resistant CVB3 Nancy. Furthermore, pleconaril with 3-methyl, 3-methoxy, 3-bromine, 2,3-dimethyl in the central ring as well as the external rings in meta position were synthesized for structure-activity relationship analysis with CVB3 variants containing leucine, methionine or isoleucine at position 1092, other coxsackieviruses B (CVB) as well as several rhinoviruses. The results demonstrate a high impact of substituents in the central ring of capsid inhibitors for anti-enteroviral activity. Pleconaril resistance of CVB3 based on Leu1092 or Met1092 was overcome by unsubstituted analogues or by monosubstitution with 3-methyl as well as 3-bromine in the central phenyl. The 3-bromine derivative inhibited a broad spectrum of CVB and rhinoviruses.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
Schmidtke M,Wutzler P,Zieger R,Riabova OB,Makarov VAdoi
10.1016/j.antiviral.2008.09.002subject
Has Abstractpub_date
2009-01-01 00:00:00pages
56-63issue
1eissn
0166-3542issn
1872-9096pii
S0166-3542(08)00392-6journal_volume
81pub_type
杂志文章abstract：:While the combination of zidovudine and didanosine is used in HIV-infected patients with more advanced disease, the possibility of a pharmacokinetic interaction between these two drugs remains controversial. Zidovudine doses of 50, 100, and 200 mg, combined with 67, 167, and 250 mg of didanosine were evaluated in 11 a...
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pub_type： 临床试验,杂志文章,随机对照试验
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pub_type： 杂志文章,评审
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更新日期：2010-03-01 00:00:00
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更新日期：2008-08-01 00:00:00
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pub_type： 临床试验,杂志文章,随机对照试验
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