Synthesis and biological activity of 3-R-1,2,3,4-tetrahydro-β-carboline derivatives

Choline esters of N-subtituted amino acids. VIII. Synthesis and neurotropic properties of β-dimentylaminoethyl ester salts of N-(p-alkoxybenzoyl)-α,β-dehydrophenylalanines

“…The central M-and H-cholinolytic effects were evaluated by the drug influence upon the convulsions induced by arecoline (15 mg/kg, s.c.) and nicotine (8 mg/kg, i.p. ), respectively [8]. The compounds were injected intraperitoneally at a dose of up to 200 mg/kg prior to the introduction of convulsive agents or the application ot electric signal.…”

“…The anticonvulsive activity of compounds IVa-IVh were studied on white mongrel mice weighing 18-24 g by evaluating the degree of protection against the tonic extension of maximum electroshock and the degree of prevention of the clonic convulsions induced by subcutaneous corazol injections (90 mg/ kg) [8]. The central M-and H-cholinolytic effects were evaluated by the drug influence upon the convulsions induced by arecoline (15 mg/kg, s.c.) and nicotine (8 mg/kg, i.p.…”

Design, synthesis, and biological evaluation of 2‐substituted‐2,3,4,9‐tetrahydrospiro‐β‐carboline‐3‐carboxylic acid derivatives as first‐in‐class mast cell stabilizers

“…Wen et al reported that ML120B is a more selective and potent inhibitor of IKKβ than PS‐1142 and blocks LPS, TNFα, and IL‐1β in human mast cells. β‐Carboline scaffolds have been well nourished by the nature, since these compounds have prolific therapeutic potential in myriad diseases: vertigo and hearing loss, as antibiotics precursor, proliferative disorders/cancers, neurodegenerative disorders, anxiolytic, Alzheimer disease, anti‐platelet aggregation activity, phosphodiesterase‐5 inhibitory, in ischemia/reperfusion injury, benzodiazepine agonistic activity, anti ‐ convulsant, anti ‐ psychotic activity, anti‐viral . Moreover, spiro‐β‐carbolines have shown anti‐malarial, GHSR (growth hormone secretagogue receptor) related disorders…”