1. Synthesis and anti-rhinovirus activity of novel 3-[2-(pyridinyl)vinyl]substituted -2H-chromenes and -4H-chromen-4-ones
- Author
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Conti, Cinzia, Monaco, L. P., PROIETTI MONACO, Luca, and Desideri, Nicoletta
- Subjects
Rhinovirus ,Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,chromenes ,antiviral activity ,capsid binders ,rhinovirus ,chromen-4-ones ,pyridine derivatives ,Chemistry Techniques, Synthetic ,Virus Replication ,medicine.disease_cause ,Antiviral Agents ,Biochemistry ,Inhibitory Concentration 50 ,Structure-Activity Relationship ,chemistry.chemical_compound ,Capsid ,stomatognathic system ,Drug Discovery ,Pyridine ,medicine ,Humans ,Benzopyrans ,Molecular Biology ,Dose-Response Relationship, Drug ,Organic Chemistry ,virus diseases ,Small molecule ,In vitro ,chemistry ,Mechanism of action ,Molecular Medicine ,medicine.symptom ,HeLa Cells - Abstract
Human rhinoviruses (HRVs) are the most common cause of viral respiratory infections and their complications. So far, no anti-viral agent has been approved for prevention or treatment of HRV infections. Pursuing our researches on small molecules with anti-rhinovirus activity, in this paper we describe the synthesis and in vitro anti-HRV 1B and 14 properties of new [2-(2H-chromen-3-yl)vinyl]pyridines and 3-[2-(pyridinyl)vinyl]-4H-chromen-4-ones. Generally, the synthesized compounds interfered with the replication of both serotypes at the micromolar or submicromolar concentrations. Preliminary results on their mechanism of action, performed on selected (E)-2-[2-(2H-chromen-3-yl)vinyl]pyridine, indicate an interference with the early step(s) of HRV 1B and 14 replication, probably at the uncoating level.
- Published
- 2014
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