Design, synthesis and in vitro evaluation of novel chroman-4-one, chroman, and 2H-chromene derivatives as human rhinovirus capsid-binding inhibitors.

摘要: As part of an effort to generate broad-spectrum inhibitors rhinovirus replication, novel series (E)-3-[(E)-3-phenylallylidene]chroman-4-ones 1a-e, (E)-3-(3-phenylprop-2-yn-1-ylidene)chroman-4-ones 2a and 2b, (Z)-3-[(E)-3-phenylallylidene]chromans 3a-e, (E)-3-(3-phenylprop-1-en-1-yl)-2H-chromenes 4a-d were designed synthesized. All the compounds tested in vitro for their efficacy against infection by human (HRV) 1B 14, two representative serotypes group B A, respectively. Most analogues found be potent selective both HRVs, although HRV was generally more susceptible than 14. Mechanism action studies (E)-6-chloro-3-(3-phenylprop-1-en-1-yl)-2H-chromene 4b, most compound on infection, suggested that 4b behaves as a capsid-binder probably acting at uncoating level.