160657-19-2

Upstream product

• 160657-18-1 5,6-dihydro-2-benzyloxy-6-oxopyrido[3,2-e]pyrrolo[1,2-a]pyrazine 
• 27048-04-0 2-amino-6-chloro-3-nitropyridine 
• 160657-16-9 6-benzyloxy-3-nitro-2-(1-pyrrolyl)pyridine 
• 160657-17-0 3-amino-6-benzyloxy-2-(1-pyrrolyl)pyridine 
• 160657-15-8 6-(benzyloxy)-3-nitropyridin-2-amine 
• 20194-18-7 sodium phenyl-methanolate 

Relevant academic research and scientific papers

Tricyclic pyrrolopyrazine 5-HT3 -active compounds

The present invention relates to a compound selected from these of formula (I): STR1 in which A and R1 are as defined in the description, and medicinal product containing the same which is useful for treating a disorder linked to the 5-HT3 receptors.

Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines

In continuation of our previous work on piperazinopyrrolothienopyrazine derivatives, three series of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines were prepared and evaluated as 5-HT3 receptor ligands. The chemical modifications performed within these new series led to structure-activity relationships regarding both high affinity and selectivity for the 5-HT3 receptors that are in agreement with those established previously for the pyrrolothienopyrazine series. The best compound (8a) obtained in these new series is in the picomolar range of affinity for 5-HT3 receptors with a selectivity higher than 106. Four of the high-affinity 5-HT3 ligands (8a, 15a,b, and 16d) were selected in both the pyridopyrrolopyrazine and the pyrroloquinoxaline series and were characterized in vitro and in vivo as agonists or partial agonists. Compound 8a was also evaluated in the light/dark test where it showed potential anxiolytic-like activity at very low doses per os.