``Viologen'' Dendrimers as Antiviral Agents: The Effect of Charge Number and Distance

Autor(en): Asaftei, Simona
De Clercq, Erik
Stichwörter: AIDS; ASSAY; Chemistry, Medicinal; EXPRESSION; HIV-1; HTLV; HUMAN-IMMUNODEFICIENCY-VIRUS; MECHANISM; Pharmacology & Pharmacy; POTENT; REPLICATION; TYPE-1
Erscheinungsdatum: 2010
Herausgeber: AMER CHEMICAL SOC
Journal: JOURNAL OF MEDICINAL CHEMISTRY
Volumen: 53
Ausgabe: 9
Startseite: 3480
Seitenende: 3488
Zusammenfassung: 
A series of ``viologen'' derivatives (4,4'-bipyridinium salts) carrying between 1 and 90 charges per molecule have been prepared and investigated for their activity against human immunodeficiency virus (HIV), herpes simplex virus (HSV), vesicular stomatitis, Punta Toro virus, Sindbis virus, Reovirus, and respiratory syncytial viruses. In general, most of the compounds showed good activities against HIV-1 (strain IIIB). In particular, compound 36 exhibited the highest in vitro activity and selectivity index against HIV-1 (strain IIIB) (EC50 = 0.26 /- 0.08 mu M, SI = 75.7) in MT-4 cells. The results imply that the antiviral activity requires an optimal number and distance of the positive charges.
ISSN: 00222623
DOI: 10.1021/jm100093p

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