Flynn G A, Ash R J
Merrell Dow Research Institute, Cincinnati, Ohio 45215.
Biochem Biophys Res Commun. 1990 Jan 30;166(2):673-80. doi: 10.1016/0006-291x(90)90862-h.
A novel route to activated phenolic sulfoxide analogs of sparsomycin has been developed. These analogs display an enhanced "preincubation effect" as inhibitors of peptide-bond formation. This time-dependent component of inhibition, which is postulated to result from an enzyme-mediated Pummerer rearrangement, is the dominant route to inhibition in these activated analogs.
已开发出一种合成司帕索霉素活性酚亚砜类似物的新途径。这些类似物作为肽键形成抑制剂表现出增强的“预孵育效应”。这种抑制的时间依赖性成分被认为是由酶介导的普默勒重排导致的,是这些活性类似物中抑制作用的主要途径。