Novel, orally effective cyanide antidotes
Novel, orally effective cyanide antidotes
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DOI：
10.1021/jm7011497
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发表时间：
2007-12-27
影响因子：
7.3
通讯作者：
Patterson, Steven E.
中科院分区：
文献类型：
--
作者：
Nagasawa, Herbert T.;Goon, David J. W.;Patterson, Steven E.
3-巯基丙酮酸（3-MP）是3-巯基丙酮酸/氰化物硫转移酶（3-MPST）的底物，可将氰化物转化为无毒的硫氰酸盐，是一种高效的氰化物解毒剂。3-MP的这些前药的独特之处在于不仅是口服的。本发明的化合物具有生物可利用性，但可以在氰化物作为预防剂之前最多一小时施用，并且当胃肠外施用时，既有快速作用又有缓慢作用。
A series of prodrugs of 3-mercaptopyruvate (3-MP), the substrate for the enzyme 3-mercaptopyruvate/cyanide sulfurtransferase (3-MPST) that converts cyanide to the nontoxic thiocyanate, which are highly effective cyanide antidotes, have been developed. These prodrugs of 3-MP are unique in being not only orally. bioavailable, but may be administered up to an hour prior to cyanide as a prophylactic agent and are both rapid- or slow-acting when given parenterally.