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J Med Chem ; 48(10): 3481-91, 2005 May 19.
Artigo em Inglês | MEDLINE | ID: mdl-15887957


1H-Imidazo-[4,5-c]quinolines were prepared while investigating novel nucleoside analogues as potential antiviral agents. While these compounds showed no direct antiviral activity when tested in a number of cell culture systems, some demonstrated potent inhibition of virus lesion development in an intravaginal guinea pig herpes simplex virus-2 assay. We have determined that the in vivo antiviral activity can be attributed to the ability of these molecules to induce the production of cytokines, especially interferon (IFN), in this model. Subsequently, we found that the compounds also induce in vitro production of IFN in human peripheral blood mononuclear cells (hPBMCs). The in vitro results reported herein and the in vivo results reported previously led to the discovery of imiquimod, 26, which was developed as a topical agent and has been approved for the treatment of genital warts, actinic keratosis, and superficial basal cell carcinoma.

Aminoquinolinas/síntese química , Antivirais/síntese química , Imidazóis/síntese química , Indutores de Interferon/síntese química , Interferons/biossíntese , Quinolinas/síntese química , Aminoquinolinas/química , Aminoquinolinas/farmacologia , Animais , Antivirais/química , Antivirais/farmacologia , Linhagem Celular Tumoral , Células Cultivadas , Efeito Citopatogênico Viral/efeitos dos fármacos , Cobaias , Herpesvirus Humano 2/efeitos dos fármacos , Humanos , Imidazóis/química , Imidazóis/farmacologia , Imiquimode , Indutores de Interferon/química , Indutores de Interferon/farmacologia , Leucócitos Mononucleares/efeitos dos fármacos , Leucócitos Mononucleares/metabolismo , Quinolinas/química , Quinolinas/farmacologia , Relação Estrutura-Atividade