Abstract：
:The preparation of a series of indole N-acyl and N-carbamic esters of (+/-)-alpha-5-[1-(indol-3-yl)ethyl]-2-methylamino-delta2-thiazolin-4-one (1) is reported. These derivatives were synthesized as potential water-soluble precursors of the antiviral thiazolinone 1, for evaluation by intranasal administration against influenza and other respiratory infections caused by viruses. Salts of the basic carbamic esters (16--19) possess the required water solubility, undergo rapid hydrolysis and decarboxylation at pH values greater than 6, and have high activity against influenza A2 and Coxsackie B1 viruses in vitro. In influenza A2 infected ferrets a representative ester (16) reduced the severity and duration of disease symptoms and reduced nasal wash virus titres but caused local irritancy.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Harnden MR,Bailey S,Boyd MR,Wilkinson JB,Wright NDdoi
10.1021/jm00188a013subject
Has Abstractpub_date
1979-02-01 00:00:00pages
191-5issue
2eissn
0022-2623issn
1520-4804journal_volume
22pub_type
杂志文章abstract：:Sepsis, which is a systemic inflammatory response that follows a bacterial infection, has a high mortality rate and limited therapeutic options. Here we show that the antimicrobial peptide OH-CATH30, which naturally occurs in snake, selectively regulates the innate immune response to protect mice from lethal sepsis. T...
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更新日期：2015-03-26 00:00:00
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