Courtoison J C, Coudert P, Couquelet J, Tronche P, Jonadet M, Bastide P
Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, Université de Clermont-Ferrand, France.
Farmaco Sci. 1988 Feb;43(2):153-60.
Using two routes starting from cyclanones, it has been possible to prepare two series of spirohydantoins substituted or not on the hydantoin nucleus nitrogen. These compounds exhibited low toxicity on pig lens aldose reductase (except for two compounds). A discussion is given on the steric and geometric requirements for effective enzyme inhibiting activity.
从环烷酮出发通过两条路线,已能够制备出两类在乙内酰脲核氮原子上有或没有取代基的螺乙内酰脲。这些化合物对猪晶状体醛糖还原酶表现出低毒性(除了两种化合物)。文中对有效酶抑制活性的空间和几何要求进行了讨论。