Delaet N G J, Robinson L A, Wilson D M, Sullivan R W, Bradley E K, Dankwardt S M, Martin R L, Van Wart H E, Walker K A M
CombiChem Inc., 4570 Executive Drive, 92121, San Diego, CA, USA.
Bioorg Med Chem Lett. 2003 Jul 7;13(13):2101-4. doi: 10.1016/s0960-894x(03)00404-9.
The parallel synthesis of novel inhibitors of procollagen C-terminal proteinase is described. The synthetic strategy allowed for the facile synthesis of a large number of side-chain diversified diamino acid hydroxamates, of which the D-diaminopropionic acid derivatives were shown to be single digit nanomolar PCP inhibitors.
本文描述了前胶原C末端蛋白酶新型抑制剂的平行合成。该合成策略使得大量侧链多样化的二氨基酸异羟肟酸酯能够简便合成,其中D-二氨基丙酸衍生物被证明是纳摩尔级的前胶原C末端蛋白酶(PCP)抑制剂。