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N-Alkylated aminopyrazines for use as hydrophilic optical agents

机译：N-烷基化氨基吡嗪用作亲水性光学试剂

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Rapid assessment of glomerular filtration rate (GFR), which measures the amount of plasma filtered through the kidney within a given time, would greatly facilitate monitoring of renal function for patients at the bedside in the clinic. In our pursuit to develop exogenous fluorescent tracers for real-time monitoring of renal function by optical methods, Nalkylated aminopyrazine dyes and their hydrophilic conjugates based on poly (ethylene glycol) (PEG) were synthesized via reductive amination as the key step. Photophysical properties indicated a bathochromic shift on the order of 50 nm in both absorption and emission compared to naked aminopyrazines which could be very useful in enhancing both tissue penetration as well as easier detection methods. Structure–activity relationship (SAR) and pharmacokinetic (PK) studies, and the correlation of in vivo optical data with plasma PK for measurement of clearance (and hence GFR) are focus of the current investigation.
机译：快速评估肾小球过滤速率（GFR），该肾小球过滤速率（GFR）测量通过肾脏在给定时间内通过肾脏过滤的血浆量将极大地促进诊所床边患者的肾功能监测。在我们追求开发外源性荧光示踪剂时，通过光学方法实时监测肾功能，通过作为关键步骤的还原胺化合成基于聚（乙二醇）（PEG）的Nalkylate氨基吡嗪染料及其基于聚（乙二醇）（PEG）的亲水缀合物。与裸氨基甲酰胺相比，光学性特性在吸收和排放中，在吸收和排放量的阶阶偏移量表示，这对于提高组织渗透以及更容易的检测方法，这是非常有用的。结构 - 活性关系（SAR）和药代动力学（PK）研究，以及具有等离子体PK的体内光学数据的相关性，用于测量间隙（并且因此GFR）是电流调查的焦点。

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