Synthesis and biologic distribution of mercapto derivatives of palmitic acid.
Synthesis and biologic distribution of mercapto derivatives of palmitic acid.
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棕榈酸巯基衍生物的合成和生物分布。
DOI：
10.1021/jm00191a024
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发表时间：
1979
影响因子：
7.3
通讯作者：
V. Warner
中科院分区：
文献类型：
--
作者：
E. Livni;M. A. Davis;V. Warner
棕榈酸的巯基衍生物能够结合99 mTc。基于99 mTc标记的棕榈酸衍生物的生物学行为类似于棕榈酸，因此可以用作心肌显像剂的假设，已经制备了三种巯基棕榈酸衍生物。以2-巯基棕榈酸、2-巯基-1，16-十六烷二酸和16-巯基棕榈酸为原料，分别与硫脲反应合成了相应的溴代化合物。在热致心肌梗塞的大鼠中评价35 S-标记的化合物和[16- 14 C]棕榈酸，以研究引入巯基基团的效果。2-[35 S]巯基棕榈酸的器官分布与[16- 14 C]棕榈酸最相似。
Mercapto derivatives of palmitic acid are capable of binding 99mTc. Based on the hypothesis that 99mTc-labeled palmitic acid derivatives would behave biologically like palmitic acid and thus could be used as myocardial imaging agents, three mercaptopalmitic acid derivatives have been prepared. The synthesis of 2-mercaptopalmitic acid, 2-mercapto-1,16-hexadecanedioic acid, and 16-mercaptopalmitic acid was accomplished by reaction of the corresponding bromo compound with thiourea. The 35S-labeled compounds and [16-14C]palmitic acid were evaluated in rats with a heat-inflicted myocardial infarction to study the effect of the introduction of the mercapto group. The organ distribution of 2-[35S]mercaptopalmitic acid was most similar to that of [16-14C]palmitic acid.