2905-60-4Relevant articles and documents
Synthesis of stable isotopically labelled versions of Lamotrigine and its methylated metabolite
Manning, Calvin O.,Wadsworth, Alan H.,Fellows, Ian
, p. 611 - 618 (2002)
Lamotrigine is a sodium channel antagonist used for the treatment of epilepsy. Synthesis of stable isotopically labelled (SIL) [M + 7] versions of Lamotrigine (1) and its N-methylated metabolite (2) are described. The routes to prepare these compounds used [M + 5] labelled [13C, 15N4]-aminoguanidine (obtained from labelled thiourea). The overall yield for the metabolite (2) was 34% from [M + 3] labelled [13C, 15N2]-thiourea. Copyright
Synthesis and anti-rheumatoid arthritis activities of 3-(4-aminophenyl)-coumarin derivatives
Miao, Yuhang,Yang, Jie,Yun, Yinling,Sun, Jie,Wang, Xiaojing
, p. 450 - 461 (2021/02/19)
Rheumatoid arthritis is a chronic systemic disease characterised by an unknown aetiology of inflammatory synovitis. A large number of studies have shown that synoviocytes show tumour-like dysplasia in the pathological process of RA, and the changes in the expression of related cytokines are closely related to the pathogenesis of RA. In this thesis, a series of novel 3-(4-aminophenyl) coumarins containing different substituents were synthesised to find new coumarin anti-inflammatory drugs for the treatment of rheumatoid arthritis. The results of preliminary activity screening showed that compound 5e had the strongest inhibitory activity on the proliferation of fibroid synovial cells, and it also had inhibitory effect on RA-related cytokines IL-1, IL-6, and TNF-α. The preliminary mechanism study showed that compound 5e could inhibit the activation of NF-κB and MAPKs signal pathway. The anti-inflammatory activity of compound 5ein?vivo was further determined in the rat joint inflammation model.
Synthesis and biological evaluation of 3–(4-aminophenyl)-coumarin derivatives as potential anti-Alzheimer’s disease agents
Hu, Yu-Heng,Yang, Jie,Zhang, Yun,Liu, Ke-Chun,Liu, Teng,Sun, Jie,Wang, Xiao-Jing
, p. 1083 - 1092 (2019/06/06)
The work is focused on the design of drugs that prevent and treat Alzheimer’s disease (AD) and its complications. A series of 3–(4-aminophenyl)-coumarin derivatives designed, synthesised, fully characterised and evaluated in vitro/vivo. The biological assay experiments showed that some compounds displayed a clearly selective inhibition for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among all compounds, compound 4m exhibited the highest AChE inhibition with an IC50 value of 0.091 ± 0.011 μM and compound 4k exhibited the highest BuChE inhibition with an IC50 value of 0.559 ± 0.017 μM. A zebrafish behaviour analyser (Zebrobox) was used to determine the behavioural effects of the active compound on the movement distance of the aluminium chloride-induced zebrafish. Compound 4m offered a potential drug design concept for the development of therapeutic or preventive agents for AD and its complications.