1134963-69-1Relevant articles and documents
Synthesis and biological evaluation of amidine, guanidine, and thiourea derivatives of 2-amino-(6-trifluoromethoxy)benzothiazole as neuroprotective agents potentially useful in brain diseases
Anzini, Maurizio,Chelini, Alessia,Mancini, Alessandra,Cappelli, Andrea,Frosini, Maria,Ricci, Lorenzo,Valoti, Massimo,Magistretti, Jacopo,Castelli, Loretta,Giordani, Antonio,Makovec, Francesco,Vomero, Salvatore
, p. 734 - 744 (2010)
A series of amidine, thiourea, and guanidine derivatives of 2-amino-6-(trifluoromethoxy)benzothiazole termed 2, 3, and 4, respectively, and structurally related to riluzole, a neuroprotective drug in many animal models of brain disease, have been synthesized. The biological activity of compounds 2a-e, 3a-f, and 4a,b was preliminarily tested by means of an in vitro protocol of ischemia/reperfusion injury. The results demonstrated that 2c and 3a-d significantly attenuated neuronal injury. Selected for testing of their antioxidant properties, compounds 3a-d were shown to be endowed with a direct ROS scavenging activity. Compounds 3b and 3d were also evaluated for their activity on voltage-dependent Na+ and Ca2+ currents in neurons from rat piriform cortex. At 50 μM, compound 3b inhibited the transient Na+ current to a much smaller extent than riluzole, whereas 3d was almost completely ineffective. 2009 American Chemical Society.
