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Sulfonyl-Containing Boronate Caps for Optimization of Biological Properties of 99mTc(III) Radiotracers [99mTcCl(CDO)(CDOH)2B-R] (CDOH2 = Cyclohexanedione Dioxime)
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-12-27 00:00:00 , DOI: 10.1021/acs.jmedchem.7b01412 Zuo-Quan Zhao 1 , Min Liu 2 , Wei Fang 1 , Shuang Liu 2
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-12-27 00:00:00 , DOI: 10.1021/acs.jmedchem.7b01412 Zuo-Quan Zhao 1 , Min Liu 2 , Wei Fang 1 , Shuang Liu 2
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In this study, different boronate caps were used to optimize biodistribution properties of radiotracers [99mTcCl(CDO)(CDOH)2B-R] (1, R = 3S; 2, R = 3SP; 3, R = 3MS; 4, R = 3DMS; 5, R = 3MSB; 6, R = 3MMS; 7, R = 3MSA; 8, R = 3DMSA; 9, R = 4S; 10, R = 4MS; 11, R = 4MSB). Among the 11 new 99mTc radiotracers, 2 shows the most promising characteristics of an optimal heart imaging agent. Its initial heart uptake is close to that of 99mTc-Teboroxime, but its heart retention time is significantly longer. Its heart/liver, heart/lung, and heart/muscle ratios are also better than those of 99mTc-Teboroxime. The SPECT image quality with 2 in SD rats is better than that with 99mTc-Teboroxime. The high initial heart uptake, long heart retention, and high heart/background ratios make 2 an excellent SPECT radiotracer for MPI.
中文翻译：
用于优化99m Tc（III）放射性示踪剂[ 99m TcCl（CDO）（CDOH）2 B-R]（CDOH 2 =环己二酮二肟）的生物学性质的含磺酰基硼酸酯盖。
在这项研究中，使用了不同的硼酸盐盖来优化放射性示踪剂的生物分布特性[ 99m TcCl（CDO）（CDOH）2 B-R]（1，R = 3S；2，R = 3SP；3，R = 3MS；4，R = 3DMS；5，R ＝ 3MSB；6，R ＝ 3MMS；7，R ＝ 3MSA；8，R ＝ 3DMSA；9，R ＝ 4S；10，R ＝ 4MS；11，R ＝ 4MSB）。在11种新的99m Tc放射性示踪剂中，有2种表现出最佳心脏成像剂的最有希望的特征。最初的心脏摄取量接近99mTc-四硼环肟，但其心脏保留时间明显更长。它的心/肝，心/肺和心/肌比也优于99m Tc-四硼肟。SD大鼠中SPECT的图像质量为2，优于99m Tc-Teboroxime。高初始心脏摄取，长心脏保留和高心脏/背景比率使2成为MPI的出色SPECT放射性示踪剂。
更新日期：2017-12-27
中文翻译：
用于优化99m Tc（III）放射性示踪剂[ 99m TcCl（CDO）（CDOH）2 B-R]（CDOH 2 =环己二酮二肟）的生物学性质的含磺酰基硼酸酯盖。
在这项研究中，使用了不同的硼酸盐盖来优化放射性示踪剂的生物分布特性[ 99m TcCl（CDO）（CDOH）2 B-R]（1，R = 3S；2，R = 3SP；3，R = 3MS；4，R = 3DMS；5，R ＝ 3MSB；6，R ＝ 3MMS；7，R ＝ 3MSA；8，R ＝ 3DMSA；9，R ＝ 4S；10，R ＝ 4MS；11，R ＝ 4MSB）。在11种新的99m Tc放射性示踪剂中，有2种表现出最佳心脏成像剂的最有希望的特征。最初的心脏摄取量接近99mTc-四硼环肟，但其心脏保留时间明显更长。它的心/肝，心/肺和心/肌比也优于99m Tc-四硼肟。SD大鼠中SPECT的图像质量为2，优于99m Tc-Teboroxime。高初始心脏摄取，长心脏保留和高心脏/背景比率使2成为MPI的出色SPECT放射性示踪剂。
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