Mazhani L, Kim B C, Poillon W N
Hemoglobin. 1984;8(2):129-36. doi: 10.3109/03630268408991706.
The effects of various tetrasubstituted ammonium compounds on the solubility of deoxygenated sickle hemoglobin were evaluated. These conclusions were drawn from the slopes of the solubility profiles obtained: (1) for the homologous series of tetraalkylammonium chloride salts (R4NCl), antigelling potency increased with increasing chain length of the R group: Ch3 less than C2H5 less than C3H7 less than C4H9; (2) for halide salts of the tetrabutylammonium cation there was no difference in effectiveness among the anions examined (Br-, Cl-, F-), presumably because of the extremely potent salting-in effect of this cation; (3) substitution of a benzyl for an alkyl group in three tetraalkylammonium chloride salts, C6H5CH2(R)3NCl, where R = CH3, C2H5, or C4H9, potentiated the antigelling capacity by as much as eight-fold. Because they are substantially more water soluble than any other class of noncovalent inhibitors examined to date, further manipulation of the aryl substituent on these compounds may contribute to the design of an effective antisickling agent.
评估了各种四取代铵化合物对脱氧镰状血红蛋白溶解度的影响。这些结论是根据所获得的溶解度曲线的斜率得出的：（1）对于四烷基氯化铵盐（R4NCl）的同系物系列，抗凝胶化能力随R基团链长的增加而增强：CH3 < C2H5 < C3H7 < C4H9；（2）对于四丁基铵阳离子的卤化物盐，在所研究的阴离子（Br-、Cl-、F-）之间有效性没有差异，推测是由于该阳离子极强的盐溶效应；（3）在三种四烷基氯化铵盐C6H5CH2(R)3NCl中，用苄基取代烷基，其中R = CH3、C2H5或C4H9，抗凝胶化能力增强了多达八倍。由于它们比迄今为止研究的任何其他类别的非共价抑制剂在水中的溶解度都要大得多，对这些化合物上芳基取代基的进一步操作可能有助于设计出有效的抗镰变剂。
