Selection of an oral prodrug (BRL 42810; famciclovir) for the antiherpesvirus agent BRL 39123 [9-(4-hydroxy-3-hydroxymethylbut-l-yl)guanine; penciclovir]
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منابع مشابه
Antiherpesvirus activity of 9-(4-hydroxy-3-hydroxymethylbut-1-yl) guanine (BRL 39123) in animals.
The antiviral activity of 9-(4-hydroxy-3-hydroxymethylbut-1-yl)guanine (BRL 39123) was assessed in several animal models of herpes simplex virus (HSV) infection. BRL 39123 was as active as acyclovir (ACV) when applied topically to guinea pigs with a cutaneous HSV type 1 (HSV-1) infection and was also active topically in an HSV-2 genital infection. Before systemic administration to infected anim...
متن کاملIn vitro antiviral activity of penciclovir, a novel purine nucleoside, against duck hepatitis B virus.
The in vitro antihepadnavirus activities of the purine nucleoside analogs ganciclovir (9-[2-hydroxy-1-(hydroxymethyl)ethoxymethyl]guanine) and penciclovir [9-(4-hydroxy-3-hydroxymethylbut-1-yl)guanine; BRL 39123] were compared in primary duck hepatocyte cultures congenitally infected with the duck hepatitis B virus (DHBV). Both compounds inhibited DHBV DNA replication to a comparable extent dur...
متن کاملShort Communication PHARMACOKINETIC STUDIES OF 2-AMINO-9-(3-ACETOXYMETHYL-4- ISOPROPOXYCARBONYL-OXYBUT-1-YL)PURINE, AN ORAL PRODRUG FOR THE ANTIVIRAL AGENT PENCICLOVIR
2-Amino-9-(3-acetoxymethyl-4-isopropoxycarbonyloxybut-1-yl)purine (SK1899) was tested as an oral prodrug for penciclovir. SK1899 was administered orally to rats and dogs at doses up to 2 and 0.68 mmol/kg, respectively. SK1899 was well absorbed, and the major metabolites detected in plasma and urine were penciclovir, the active antiviral compound, and 6-deoxypenciclovir (M4) in both species. In ...
متن کاملPharmacokinetic studies of 2-amino-9-(3-acetoxymethyl-4-isopropoxycarbonyl-oxybut-1-yl)purine, an oral prodrug for the antiviral agent penciclovir.
2-Amino-9-(3-acetoxymethyl-4-isopropoxycarbonyloxybut-1-yl)- purine (SK1899) was tested as an oral prodrug for penciclovir. SK1899 was administered orally to rats and dogs at doses up to 2 and 0.68 mmol/kg, respectively. SK1899 was well absorbed, and the major metabolites detected in plasma and urine were penciclovir, the active antiviral compound, and 6-deoxypenciclovir (M4) in both species. I...
متن کاملBRL.8988 (talampicillin), a well-absorbed oral form of ampicillin.
The phthalidyl ester (BRL.8988, talampicillin) of ampicillin gave serum levels in man two and a half times those obtained with ampicillin itself.
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ژورنال
عنوان ژورنال: Antimicrobial Agents and Chemotherapy
سال: 1989
ISSN: 0066-4804,1098-6596
DOI: 10.1128/aac.33.10.1765