Parker G R, Moore E C
J Pharm Sci. 1977 Jul;66(7):1040-4. doi: 10.1002/jps.2600660737.
The carbonyl nitrogen IR absorption region of selected hydroxyureas was examined in octanol. The spectra indicated appreciably different absorptions prior to and after equilibration with water. Stability studies on the hydroxyureas indicated that the absorption differences were not due to chemical decomposition in the equilibration process but were due to solvent conformation and/or tautomeric dependency of the system. Preliminary in vitro inhibition of the enzyme ribonucleoside diphosphate reductase by selected hydroxyureas also indicated an apparent solvent dependency, which may involve the conformational and/or tautomeric properties of these agents. The implications of the solvent-dependent conformation-tautomeric system observed are discussed in relation to this property in the biological action of these agents.
在辛醇中对选定的羟基脲的羰基氮红外吸收区域进行了检测。光谱表明，与水达到平衡前后的吸收存在明显差异。对羟基脲的稳定性研究表明，吸收差异并非由于平衡过程中的化学分解，而是由于体系的溶剂构象和/或互变异构依赖性。选定的羟基脲对核糖核苷二磷酸还原酶的初步体外抑制作用也表明存在明显的溶剂依赖性，这可能涉及这些药物的构象和/或互变异构性质。结合这些药物生物作用中的这一特性，讨论了所观察到的溶剂依赖性构象-互变异构体系的影响。
