516445-83-3Relevant articles and documents
Synthesis and identifications of potential metabolites as biomarkers of the synthetic cannabinoid AKB-48
Wallgren, Jakob,Vikingsson, Svante,?strand, Anna,Josefsson, Martin,Gréen, Henrik,Dahlén, Johan,Wu, Xiongyu,Konradsson, Peter
, p. 2905 - 2913 (2018)
AKB-48 belongs to the family of synthetic cannabinoids. It has strong binding affinity to CB1 receptor and is psychoactive. It is banned in many countries including USA, Japan, Germany, New Zealand, Singapore and China etc. But the difficulty in detecting the parent compound in urine samples highlights the importance of studies of its metabolites. Here we report the synthesis of 19 potential metabolites of AKB-48, among which, compounds 2, 9, 10, 30 and 31, together with the commercially available substance 5 were identified as metabolites of AKB-48 by comparison with one authentic human urine sample and human liver microsomal data. Compounds 10 and 30 could be of use as biomarkers in detecting AKB-48 in human urine samples.
Azaindole derivative and preparation method and application thereof
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Paragraph 0167-0168, (2020/08/30)
The invention belongs to the technical field of medicines, and discloses an azaindole derivative shown as a formula (I) and/or a medicinal salt and a preparation method thereof. The preparation methodcomprises the following steps: carrying out amidation reaction on a compound shown as a formula (II) and amantadine to obtain a compound shown as a formula (III); and carrying out nucleophilic substitution reaction on the compound shown in the formula (III) and halogenated R1 to obtain the compound shown in the formula (I). The azaindole-2-formamide derivative is an agonist with high selectivity,high affinity and high activity on a cannabinoid type 2 receptor (CB2), and the structural formula of the azaindole-2-formamide derivative is shown in the specification. The active prevention and treatment effects can be achieved on multiple sclerosis, autoimmune diseases, osteoporosis, neurodegeneration, organ transplantation immunological rejection, tumor resistance and other various cannabinoid receptor related diseases.
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents
Joubert, Jacques,Dyk, Sandra Van,Green, Ivan R.,Malan, Sarel F.
experimental part, p. 3935 - 3944 (2011/08/06)
A series of fluorescent heterocyclic adamantane amines were synthesised with the goal to develop novel fluorescent ligands for neurological assay development. These derivatives demonstrated multifunctional neuroprotective activity through inhibition of the N-methyl-d-aspartate receptor/ion channel, calcium channels and the enzyme nitric oxide synthase. It also exhibited a high degree of free radical scavenging potential. N-(1-adamantyl)-2-oxo-chromene-3- carboxamide (8), N-adamantan-1-yl-5-dimethyl-amino-1-naphthalenesulfonic acid (11) and N-(1-cyano-2H-isoindol-2-yl) adamantan-1-amine (12) were found to possess a high degree of multifunctionality with favourable physical-chemical properties for bioavailability and blood-brain barrier permeability. The ability of these heterocyclic adamantane amine derivatives as nitric oxide synthase inhibitors, calcium channel modulators, NMDAR inhibitors and effective antioxidants, indicate that they may find application as multifunctional drugs in neuroprotection.
