Elfarra A A, Yeh H, Hanna P E
J Med Chem. 1982 Oct;25(10):1189-92. doi: 10.1021/jm00352a018.
N-(4-Phenylcyclohexyl)acetohydroxamic acid and a series of N-(phenylalkyl)acetohydroxamic acids were synthesized and evaluated as substrates for partially purified rat and hamster hepatic arylhydroxamic acid N,O-acyltransferase systems (AHAT). The compounds were assayed for their abilities to function as acetyl donors in the AHAT-mediated transacetylation of 4-aminoazobenzene and for their abilities to participate in the AHAT-mediated conversion of N-arylhydroxylamines to electrophilic intermediates that form methylthio adducts upon reaction with N-acetylmethionine. None of the newly synthesized compounds displayed significant activity in either of the assays. The results of this study indicate that acetohydroxamic acids that have the nitrogen atom of the hydroxamic acid group attached directly to aliphatic or cycloalkyl groups are not likely to serve as substrates or inhibitors of AHAT.
合成了N-(4-苯基环己基)乙酰氧肟酸及一系列N-(苯基烷基)乙酰氧肟酸，并将其作为大鼠和仓鼠肝脏部分纯化的芳基氧肟酸N,O-酰基转移酶系统（AHAT）的底物进行评估。测定了这些化合物在AHAT介导的4-氨基偶氮苯转乙酰化反应中作为乙酰供体的能力，以及它们参与AHAT介导的N-芳基羟胺转化为亲电中间体（该中间体与N-乙酰甲硫氨酸反应形成甲硫基加合物）的能力。在任何一种测定中，新合成的化合物均未表现出显著活性。本研究结果表明，羟肟酸基团的氮原子直接连接到脂肪族或环烷基上的乙酰氧肟酸不太可能作为AHAT的底物或抑制剂。
