Department of Pharmacology and Toxicology, The University of Arizona, Tucson, AZ 85724, USA.
Molecules. 2012 May 8;17(5):5346-62. doi: 10.3390/molecules17055346.
We prepared a series of peptide-like 14-membered macrocycles containing an imidazole-4,5-dicarboxylic acid scaffold by using known coupling reagents and protecting group strategies. Yields of the purified macrocycles were poor on average, yet seemingly independent of amino acid substitution or stereochemistry. The macrocycles retain some level of conformational variability as observed by both molecular modeling and X-ray crystallography. These macrocycles represent a new class of structures for further development and for future application in high-throughput screening against a variety of biological targets.
我们使用已知的偶联试剂和保护基策略，制备了一系列含有咪唑-4,5-二羧酸骨架的肽状 14 元大环化合物。尽管平均而言，这些大环化合物的纯化产率较低，但似乎与氨基酸取代或立体化学无关。分子建模和 X 射线晶体学都表明，这些大环化合物保留了一定程度的构象可变性。这些大环化合物代表了一类新的结构，可进一步开发，并在未来应用于针对各种生物靶标的高通量筛选。
