[Synthesis and pharmacologic study of several spirohydantoins: relation to conformation].

Il Farmaco; edizione scientifica Pub Date : 1988-02-01
J C Courtoison, P Coudert, J Couquelet, P Tronche, M Jonadet, P Bastide
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Abstract

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.

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[几种螺旋藻毒素的合成及药理研究:与构象的关系]。
从旋流酮出发,采用两种途径,可以制得两种取代或不取代旋流酮核氮的旋流酮系列。这些化合物对猪晶状体醛糖还原酶的毒性较低(除两种化合物外)。讨论了有效酶抑制活性的空间和几何要求。
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