Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HT1A receptor agonists
文摘
1,4-dioxaspiro[4,5]dec-2-ylmethyl-amines were synthesized and tested. Oxygen/Sulphur substitution favors 5-HT1AR affinity, potency and efficacy. 14 and 15 behave as selective and potent 5-HT1AR partial agonists. 15 shows a promising neuroprotective activity in-vitro. 15 reduces significantly the linking time in Phase II at a dose of 10 mg/kg i.p.