Synthesis and biological evaluation of H2S donor ADT-OH derivatives
10.11665/j.issn.1000-5048.20170304
- VernacularTitle:硫化氢供体型ADT-OH衍生物的合成及其活性
- Author:
Yuyao LI
;
Heng SONG
;
Jian CHENG
;
Guizhen AO
- Keywords:
ADT-OH;
hydrogen sulfide donor;
synthesis;
anti-glutamic acid;
neuroprotection
- From:
Journal of China Pharmaceutical University
2017;48(3):276-281
- CountryChina
- Language:Chinese
-
Abstract:
5-(4-Hydroxyphenyl)-3H-1,2-dithiole-3-thione (ADT-OH) is a slowly releasing H2S 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 MTF 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,Yu are more potent than their parent compound ADT-OH at concentration of 1-10 μmol/L,which is worthy of further study.
