129823-18-3

Upstream product

• 5807-30-7 3,4-dichlorophenyl acetic acid 
• 129823-17-2 4,5,6,7-tetrahydrofuro<3,2-c>pyridine-4-methanol 
• 1121-46-6 2-Furan-2-yl-ethylamine 
• 18637-83-7 1,1'-oxalyldiimidazole 

Relevant academic research and scientific papers

4-[(Alkylamino)methyl]furo[3,2-c]pyridines: A new series of selective κ- receptor agonists

The synthesis of 5-(arylacetyl)-4-[(alkylamino)methyl]furo[3,2- c]pyridines (16-23, 26, 27) and their activities as κ-opioid receptor agonists are described. κ-Agonist potency was particularly sensitive to the nature of the basic moiety. In particular, in the rabbit vas deferens (κ- specific tissue), the 3-pyrrolidinol analogue 17 (IC50 = 2.7 nM) was found to be approximately 5-fold more potent than the corresponding pyrrolidine analogue 16 (IC50 = 15 nM). In the rat and hamster vasa deferentia (μ- specific and δ-specific tissues, respectively), 17 showed only weak antagonist activity (pK(B) > 5.5), underlining its selectivity for the κ- opioid receptor. The major activity for 17 is resident in the 4S,3'S-isomer 26 (rabbit vas deferens IC50 = 1.1 nM). Compound 26 displays excellent antinociceptive activity, as determined in the mouse acetylcholine-induced abdominal constriction test (ED50 = 0.001 mg/kg, sc).

Pharmaceutically useful furo[3,2-c]pyridines

Compounds are disclosed of formula (I) STR1 wherein R1 represents hydrogen, unsubstituted or substituted C1-6 alkyl, halogen, --COR4 or --CO2 R4 (where R4 represents hydrogen or unsubstituted or substituted C1-6 alkyl); R2 and R3 are the same or different and are C1-6 alkyl or C3-6 alkenyl; or --NR2 R3 forms a 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or a 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by hydroxy, C1-6 acyloxy, oxo, optionally substituted methylidene, --COR5 (where R5 represents C1-6 alkyl, OR6 or --NHR6, and R6 represents hydrogen, C1-6 alkyl, aryl or ar(C1-6)alkyl) or said ring is substituted by =NOR7 (where R7 represents C1-6 alkyl); Z represents --O-- or --S--; X represents a direct bond, --CH2 -- or --CH2 O--; Ar represents a substituted phenyl moiety; and pharmaceutically acceptable salts thereof. The compounds are indicated as useful in the treatment of pain and cerebral ischaemia. Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.