Abstract:
5-(4-Hydroxyphenyl)-3
H-1, 2-dithiole-3-thione(ADT-OH)is a slowly releasing H
2S donor with some neuroprotective effect. In order to study the structure-activity relationships, seventeen compounds(
Y1 -
Y17 )were synthesized by modification of ADT-OH at the aromatic ring position, and their structures were confirmed by
1H NMR,
13C NMR and HR-MS. Among them, 6 compounds(
Y4, Y13 -
Y17 )were novel compounds. Their effects had been evaluated on HT-22 hippocampal neuron cells damaged by glutamate with MTT method. The pharmacological results demonstrated that all the
Y compounds had potent neuroprotection at most of the tested concentrations(1-100 μmol/L). Compounds
Y1 -
Y9 and
Y11 significantly improved the survival rates of the damaged cells at 1-100 μmol/L(
P<0. 01). Specially, compounds
Y1, Y4, Y6 -
Y9, Y11 are more potent than their parent compound ADT-OH at concentration of 1-10 μmol/L, which is worthy of further study.