Picolyl Alkyl Amines As Novel Tyrosinase Inhibitors: Influence of Hydrophobicity and Substitution
作者:Punam Bandyopadhyay、Sujeetkumar Jha、S. K. Imran Ali
DOI:10.1021/jf902100k
日期:2009.10.28
was strongly dependent on the substitution on a pyridine ring, and the inhibition follows the trend of α-picolyl alkyl amines (A, D, G) < β-picolyl alkyl amines (B, E, H) < γ -picolyl alkyl amines (C, F, I). The inhibition kinetics have been investigated, and γ-substituted derivatives were found to be a mixed type of inhibitor, whereas β-substituted derivatives were found to exhibit uncompetitive inhibition
几种新的吡啶甲基烷基胺衍生物(甲-大号)的合成,和疏水性和替代对蘑菇酪氨酸酶的抑制朝向两侧单酚和二酚的活动的影响进行说明。α-,β-和γ-甲基吡啶胺既不是底物也不是抑制剂。然而,该抑制是通过引入烷基链来诱导的。抑制作用强烈依赖于吡啶环上的取代,并且抑制作用遵循以下趋势:α-吡啶甲基烷基胺(A,D,G)<β-吡啶甲基烷基胺(B,E,H)<γ-吡啶甲基烷基胺(C,F,我)。已经研究了抑制动力学,发现γ-取代的衍生物是抑制剂的混合类型,而发现β-取代的衍生物对L-DOPA的氧化表现出非竞争性的抑制作用。