Bollinger J C, Levy-Serpier J, Debord J, Penicaut B
Laboratoire de Chimie générale et analytique, Faculté des Sciences, Limoges, France.
J Enzyme Inhib. 1990;3(3):211-7. doi: 10.3109/14756369009035839.
Two phosphoric 4-nitroanilides Z2P(O)NH-phi-NO2 (A, Z = Me; B, Z = NMe2) have been prepared and purified by chromatographic techniques. Their spectral data (uv, ir and 1H-nmr) have been determined, and compared with those of other similar compounds. Their ability to inhibit acetylcholinesterase has been measured by a modification of Ellman's method. The data, as computed according to the Michaelis scheme, indicate that A is not an inhibitor, whereas B is a reversible mixed one. These differences are discussed in terms of hydrophobic interactions.
通过色谱技术制备并纯化了两种磷酸4-硝基苯胺Z2P(O)NH-phi-NO2(A,Z = 甲基;B,Z = 二甲基氨基)。测定了它们的光谱数据(紫外、红外和1H-核磁共振),并与其他类似化合物的数据进行了比较。通过对埃尔曼方法的改进来测定它们抑制乙酰胆碱酯酶的能力。根据米氏方程计算的数据表明,A不是抑制剂,而B是一种可逆的混合型抑制剂。从疏水相互作用的角度对这些差异进行了讨论。