新型细菌芳胺N-乙酰基转移酶（NATs）小分子抑制剂的合成及体外评价
Synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs).
作者信息
Brooke Edward W, Davies Stephen G, Mulvaney Andrew W, Okada Minoru, Pompeo Frédérique, Sim Edith, Vickers Richard J, Westwood Isaac M
机构信息
Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, UK.
出版信息
Bioorg Med Chem Lett. 2003 Aug 4;13(15):2527-30. doi: 10.1016/s0960-894x(03)00484-0.
The synthesis and inhibitory activity of a series of 5-substituted-(1,1-dioxo-2,3-dihydro-1H-1 lambda(6)-benzo[e][1,2]thiazin-4-ylidene)-thiazolidine-2,4-dione derivatives as competitive inhibitors of recombinant bacterial arylamine-N-acetyltransferases (NATs) are described. The most potent NAT inhibitors are those that contain planar hydrophobic substituents on the sultam nitrogen.
本文描述了一系列5-取代-(1,1-二氧代-2,3-二氢-1H-1λ(6)-苯并[e][1,2]噻嗪-4-亚基)-噻唑烷-2,4-二酮衍生物作为重组细菌芳胺-N-乙酰转移酶（NATs）竞争性抑制剂的合成及抑制活性。最有效的NAT抑制剂是那些在磺内酰胺氮上含有平面疏水取代基的化合物。
Zotero 插件