Masereel B, Dogné J M, Damas J, Nuhrich A, Varache-Lembège M, Fontaine J, Pochet L, Somers F, de Tullio P, Pirotte B, Delarge J
Department of Medicinal Chemistry, University of Liège.
J Pharm Belg. 1997 Jul-Aug;52(4):157-8.
Pharmacomodulation of torasemide, a diuretic sulfonylurea, led to the discovery of two novel diuretics, a sulfonylthiourea (BM 20) and a sulfonylcyanoguanidine (BM 106). BM 27, a lipophilic sulfonylurea, exhibited neuroprotective properties associated to an anticonvulsant activity. As BM 27, two lipophilic sulfonythioureas (BM 11 and BM 34) revealed an anticonvulsant profile similar to that of phenytoin. Finally the synthesis of torasemide derivatives led to the development of a sulfonylcyanoguanidine (BM 144) with a thromboxane A2 antagonist potency.
托拉塞米（一种利尿磺酰脲类药物）的药效调节导致发现了两种新型利尿剂，一种是磺酰硫脲（BM 20），另一种是磺酰氰基胍（BM 106）。BM 27是一种亲脂性磺酰脲，具有与抗惊厥活性相关的神经保护特性。与BM 27一样，两种亲脂性磺酰硫脲（BM 11和BM 34）显示出与苯妥英钠相似的抗惊厥谱。最后，托拉塞米衍生物的合成导致开发出一种具有血栓素A2拮抗剂效力的磺酰氰基胍（BM 144）。
