RESUMEN
A series of C-2 pyrroloquinoline analogs designed to improve aqueous solubility were examined for herpesvirus polymerase and antiviral activity. Several analogs were identified that maintained the antiviral activity of the previous development candidate against HCMV, HSV-1 and VZV, but with significantly improved aqueous solubility.
Asunto(s)
Antivirales/química , Herpesviridae/enzimología , Inhibidores de la Síntesis del Ácido Nucleico , Pirroles/química , Quinolinas/química , Antivirales/síntesis química , Antivirales/farmacología , Citomegalovirus/efectos de los fármacos , ADN Polimerasa Dirigida por ADN/metabolismo , Herpesvirus Humano 1/efectos de los fármacos , Herpesvirus Humano 3/efectos de los fármacos , Humanos , Pirroles/síntesis química , Pirroles/farmacología , Quinolinas/síntesis química , Quinolinas/farmacología , Solubilidad , Relación Estructura-ActividadRESUMEN
The chemoselective allylation of acetals using allyltrimethylsilane in ionic liquids is catalyzed by TMS triflate (5.0-20.0 mol %). The reaction proceeds smoothly at room temperature to afford the corresponding homoallyl ether in good yield. Since the ionic liquids are easily recovered and recycled, they are a useful alternative to dichloromethane, which is the commonly used solvent for allylations. [reaction--see text]
