Liquid chromatographic analysis of enviradene, a new antiviral agent, in plasma and its application in bioavailability studies in the dog.

  title={Liquid chromatographic analysis of enviradene, a new antiviral agent, in plasma and its application in bioavailability studies in the dog.},
  author={R. Bopp and J. F. Quay and R. M. Morris and J. F. Stucky and D. Miner},
  journal={Journal of pharmaceutical sciences},
  volume={74 8},
A rapid and specific high-performance liquid chromatographic (HPLC) assay has been developed for the determination of enviradene, 1, at concentrations of 2-5 ng/mL in plasma. The drug was extracted from the samples using benzene. The benzene extract was evaporated and the residue dissolved in the mobile phase. The HPLC system consisted of a reversed-phase column and a 75% methanol:25% 0.2 M sodium acetate mobile phase. Either a UV detector set at 268 nm or an electrochemical (EC) detector set… Expand
The effects of antirhino- and enteroviral vinylacetylene benzimidazoles on cytochrome P450 function and hepatic porphyrin levels in mice.
While all four selected compounds displayed potent antiviral activity and two of the compounds exhibited acceptable pharmacokinetic properties, the hepatic effects of these latter two compounds suggest the potential for drug induced porphyria with multidose therapeutic use. Expand
Benzimidazole derivative M084 extends the lifespan of Caenorhabditis elegans in a DAF-16/FOXO-dependent way
The results showed that M084 could extend the lifespan of C. elegans, delay age-related decline of phenotypes, and improve stress resistance, and provide clue for developing novel anti-aging agents. Expand
Synthesis of 6-[(hydroxyimino)phenyl)]methyl]-1-[(1-methylethyl)sulfonyl]-1H-imidazo[4,5-b]pyridin-2-amine. An aza analogue of enviroxime
6-[[(Hydroxyimino)phenyl]methyl]-1-[(1-methylethyl)sulfonyl]-1H-imidazo[4,5-b]pyridin-2-amine (1), an aza analogue of enviroxime, was synthesized in eight steps from 6-hydroxynicotinic acid (2). AcidExpand
先导化合物结构优化是新药研发的关键环节。通过改变先导化合物的代谢途径可以改善化合物的药代动力学特性, 延长药物在体内的作用时间, 增强代谢稳定性, 提高生物利用度。本文主要综述了通过改变代谢途径提高代谢稳定性的先导化合物结构优化策略, 包括封闭代谢位点、降低脂溶性、骨架修饰、生物电子等排以及前药等。


Determination of enviroxime in a variety of biological matrixes by liquid chromatography with electrochemical detection.
This method has proven to be applicable and reliable for the determination of enviroxime in many types of biological samples and several problems encountered during the routine use of electrochemical detection were explored and minimized. Expand
High-performance liquid chromatography with Ag+ complexation in the mobile phase
Summary By reversed-phase high-performance liquid chromatography (HPLC) on chemically bonded phases using common mobile phases (methanol-water, methanol-isopropanol, water-acetonitrile) containing AgExpand
Comparison of the antiviral effects of substituted benzimidazoles and guanidine in vitro and in vivo
It was found that the substituted benzimidazoles LY122771-72 and LY127123, when given daily for 9 days, could save significant numbers of mice from death caused by echo 9, coxsackie A9 and A16 viruses. Expand
The role of organic modifiers on polar group selectivity in reversed-phase liquid chromatography
Abstract The influence of the organic modifiers methanol (MeOH), acetonitrile (AN) and tetrahydrofuran (THF) on polar group selectivity in reversed-phase liquid chromatography has been studied. InExpand
Role of organic modifier sorption on retention phenomena in reversed-phase liquid chromatography
Abstract Distribution phenomena associated with the elution of solutes of varying retention from reversed-phase chromatographic columns have been examined. For solutes slightly more retained than theExpand
Evidence for the involvement of N-acetyl-p- quinoneimine in acetaminophen metabolism.
Evidence for the presence of N -acetyl- p -quinoneimine (NAPQI), a postulated toxic intermediate of acetaminophen metabolism, in mouse liver microsomal incubations is reported and is moderately stable at physiological pH and temperature with a lifetime which is dependent on the components of the medium. Expand
Synthesis of syn and anti isomers of 6-[[(hydroxyimino)phenyl]methyl]-1-[(1-methylethyl)sulfonyl]-1H-benzimidazol-2-amine. Inhibitors of rhinovirus multiplication.
The synthesis and antirhinovirus activity of syn and anti isomers of 6-[[(hydroxyimino)phenyl]methyl]-1-[(1-methylethyl)sulfonyl]-1H-benzimidazol-2-amine (4 and 5) are reported. The structuralExpand