55144-54-2Relevant articles and documents
Synthesis and bioactivity of substituted indan-1-ylideneaminoguanidine derivatives
Zhang, Rui,Dong, Jin,Xu, Yun-gen,Hua, Wei-yi,Wen, Na,You, Qi-dong
experimental part, p. 3771 - 3776 (2009/12/04)
In our efforts to discover more potent and lasting NHE1 inhibitors, we designed and synthesized a series of substituted indan-1-ylidene aminoguanidine derivatives (5). NHE1 inhibitory activity of twenty-one compounds 5 was evaluated in a rat platelet swelling assay. It is found that most of the tested compounds possess NHE1 inhibitory effects. 2-(5-methoxybenzimidazol-2-ylthio)-5-chloro-2,3-dihydroinden-1-ylidene aminoguanidine hydrobromide (5m) proved to be sixty-nine times more potent than cariporide. Furthermore, when tested in vivo, compound 5m also displayed superior cardioprotective effects against SD rat myocardial ischemic-reperfusion injury over those of cariporide.
IMIDAZO(1,2-A)-INDENO (1,2-E) PYRAZIN-4-ONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
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, (2008/06/13)
Pharmaceutical compositions containing, as the active principle, compounds of formula (I): STR1 wherein R, R 1 and R. sub.2 are as defined in the description, or salts thereof, the novel compounds of formula (I), and the preparation thereof. The compounds of formula (I) have valuable pharmacological properties and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, this receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NDMA) receptor antagonists, and particularly NMDA receptor glycine modulation site ligands.