首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Good oral absorption prediction on non-nucleoside benzothiadiazine dioxide human cytomegalovirus inhibitors using combined chromatographic and neuronal network techniques.
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Good oral absorption prediction on non-nucleoside benzothiadiazine dioxide human cytomegalovirus inhibitors using combined chromatographic and neuronal network techniques.

机译:使用组合的色谱和神经网络技术,对非核苷二氧化苯并噻二嗪类人巨细胞病毒抑制剂具有良好的口服吸收预测。

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摘要

The current drugs available against human cytomegalovirus (HCMV) suffer from a number of shortcomings such as toxic side effect, poor bioavailability and/or risk for emergence of drug-resistance virus strains. Due to these limitations, the development of new drugs against HCMV is of great interest. Taking into account the therapeutic potential of benzothiadiazines dioxides (BTD) derivatives, it is most important to know their oral bioavailability because all the current clinical drugs are poorly absorbed. In this work, the utility of CODES neural networks and biopartitioning micellar chromatography (BMC) in predicting pharmacokinetic properties has been used to estimate the oral absorption of BTD derivatives and their efficacy has been verified. The results indicate higher values for BTD derivatives than the currently licensed anti-viral agents.
机译:当前可用于抗人巨细胞病毒(HCMV)的药物具有许多缺点,例如毒性副作用,不良的生物利用度和/或出现抗药性病毒株的风险。由于这些限制,对HCMV的新药的开发引起了极大的兴趣。考虑到二氧化苯并噻二嗪类(BTD)衍生物的治疗潜力,最重要的是要知道它们的口服生物利用度,因为目前所有的临床药物都难以吸收。在这项工作中,已使用CODES神经网络和生物分配胶束色谱(BMC)预测药代动力学特性来评估BTD衍生物的口服吸收,并验证了其功效。结果表明BTD衍生物的价值高于当前许可的抗病毒剂。

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