Conformation constrained total synthesis macro ring compound

摘要

The conformationally constrained and spatially defined macrocycle system of formula (I) is composed of three different parts of the molecule: template A, conformation modulator B and bridge C. This ring, represented by I, is readily prepared by parallel synthesis or combinatorial chemistry in solution or in the solid phase. These compounds may interact with various classes of specific biological targets, for example: to have agonist or antagonist activity against G protein coupled receptors (GPCRs), inhibitory activity against enzymes, or antibacterial activity. Designed to. In particular, these macrocyclic compounds show inhibitory activity against subtype 1 endothelin converting enzyme (ECE-1) and / or cysteine protease cathepsin S (CatS), oxytocin (OT) receptor, thyrotropin releasing hormone (TRH) Acts as an antagonist for the receptor and / or leukotriene B4 (LTB4) receptor and / or as an agonist for the bombesin 3 (BB3) receptor and / or exhibits antibacterial activity against at least one bacterial strain. Therefore, it shows great potential as a medicine for various diseases.