A chiral HPLC and pharmacokinetic approach of 1-(4-bromophenyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-sulfonamide.

IF 1.8 4区医学 Q3 BIOCHEMICAL RESEARCH METHODS

Bioanalysis Pub Date : 2025-04-01 Epub Date: 2025-03-24 DOI:10.1080/17576180.2025.2481023

Peddaguravagari Mounika, Mariya Shelby, Chethan K S, Honnavalli Yogish Kumar, Bannimath Gurupadayya

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引用次数: 0

Abstract

Aim: The main purpose of the study is to establish Bioanalytical method development for enantiomeric divergence and Stereoselective Pharmacokinetic activity of 1-(4-bromophenyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-sulfonamide(B06).

Background: Isoquinoline derivatives have various activities like anticancer, anti-convulsant etc. The proposed project is mainly focused on anti-cancer activity of the synthesized B-06 compound as it shown very good cytotoxicity activity on MBA-MD-231 and MCF-7 cell lines by using SRB assay.

Method: The specified project was completed with HPLC and an amylose chiral column. The bioanalytical approach was developed and tested using Wister Albino rats in compliance with USFDA Guidelines and expanded to include pharmacokinetic activities.

Result: Data that had previously been published was used to design the B06 compound. RT of 9.578 and 7.076 minutes were observed for (R) &; (S) B06 Compound. Within-run and between-run precision for S-enantiomer varied from 0.28 to 6.078%, while R-enantiomer was found to range from 0.34 to 6.08%. Recovery rates ranged from 80.06% to 92.60% for both enantiomers. Pharmacokinetic investigations were developed and validated by using PKSolver software with Microsoft Excel.

Conculsion: We successfully established optimized bioanalytical method for pharmacokinetic study were both the enantiomers were properly separated. In pharmacokinetic activity we found that the enantiomers are non-stereoselective having same absorption rate.

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1-（4-溴苯基）-6,7-二甲氧基-3,4-二氢异喹啉-2(1H)-磺酰胺的手性高效液相色谱及药代动力学研究。

目的：建立1-（4-溴苯基）-6,7-二甲氧基-3,4-二氢异喹啉-2(1H)-磺酰胺（B06）对映体差异性及立体选择性药代动力学活性的生物分析方法。背景：异喹啉衍生物具有抗癌、抗惊厥等多种活性。通过SRB实验，合成的B-06化合物对MBA-MD-231和MCF-7细胞系显示出良好的细胞毒活性，本课题主要研究其抗癌活性。方法：采用高效液相色谱法和直链淀粉手性色谱柱。生物分析方法的开发和测试使用Wister白化病大鼠符合USFDA指南，并扩大到包括药代动力学活动。结果：利用先前发表的数据设计B06化合物。(R)和(R)的RT分别为9.578和7.076分钟；(S) B06化合物。s -对映体的运行内和运行间精密度范围为0.28 ~ 6.078%，r -对映体的运行内和运行间精密度范围为0.34 ~ 6.08%。两种对映体的回收率为80.06% ~ 92.60%。采用PKSolver软件和Microsoft Excel进行药代动力学研究并进行验证。结论：两种对映体分离合理，建立了优化的药代动力学研究方法。在药代动力学活性方面，我们发现对映体具有非立体选择性，具有相同的吸收率。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Bioanalysis BIOCHEMICAL RESEARCH METHODS-CHEMISTRY, ANALYTICAL

CiteScore

3.30

自引率

16.70%

发文量

审稿时长

2 months

期刊介绍： Reliable data obtained from selective, sensitive and reproducible analysis of xenobiotics and biotics in biological samples is a fundamental and crucial part of every successful drug development program. The same principles can also apply to many other areas of research such as forensic science, toxicology and sports doping testing. The bioanalytical field incorporates sophisticated techniques linking sample preparation and advanced separations with MS and NMR detection systems, automation and robotics. Standards set by regulatory bodies regarding method development and validation increasingly define the boundaries between speed and quality. Bioanalysis is a progressive discipline for which the future holds many exciting opportunities to further reduce sample volumes, analysis cost and environmental impact, as well as to improve sensitivity, specificity, accuracy, efficiency, assay throughput, data quality, data handling and processing. The journal Bioanalysis focuses on the techniques and methods used for the detection or quantitative study of analytes in human or animal biological samples. Bioanalysis encourages the submission of articles describing forward-looking applications, including biosensors, microfluidics, miniaturized analytical devices, and new hyphenated and multi-dimensional techniques. Bioanalysis delivers essential information in concise, at-a-glance article formats. Key advances in the field are reported and analyzed by international experts, providing an authoritative but accessible forum for the modern bioanalyst.