Huang, Yunsheng’s team published research in Bioorganic & Medicinal Chemistry in 2001-12-31 | CAS: 5653-62-3

Bioorganic & Medicinal Chemistry published new progress about Dopamine antagonists. 5653-62-3 belongs to class nitriles-buliding-blocks, name is 2,3-Dimethoxybenzonitrile, and the molecular formula is C9H9NO2, Name: 2,3-Dimethoxybenzonitrile.

Huang, Yunsheng published the artcileSynthesis of 2-(2,3-dimethoxyphenyl)-4-(aminomethyl)imidazole analogues and their binding affinities for dopamine D2 and D3 receptors, Name: 2,3-Dimethoxybenzonitrile, the main research area is imidazolemethanamine dimethoxyphenyl bromodimethoxyphenyl preparation dopamine receptor; imidazolylmethyl methoxyisoquinoline preparation dopamine receptor.

A series of 2-(2,3-dimethoxyphenyl)-4-(aminomethyl)imidazole derivatives was prepared and their affinity for dopamine D2 and D3 receptors was measured using in vitro binding assays. Several oxadiazole analogs were also prepared and tested for their affinity for dopamine D2 and D3 receptors. The results of receptor binding studies indicated that the incorporation of an imidazole moiety between the Ph ring and the basic nitrogen did not significantly increase the selectivity for dopamine D3 receptors, whereas the incorporation of an oxadiazole at the same region resulted in a total loss of affinity for both dopamine receptor subtype binding sites. The most selective compound in this series is 6,7-dimethoxy-2-[[2-(2,3-dimethoxyphenyl)-1H-imidazol-4-yl]methyl]-1,2,3,4-tetrahydroisoquinoline, which has a D3 receptor affinity of 21 nM and a 7-fold selectivity for D3 vs. D2 receptors. The binding affinity for σ1 and σ2 receptors was also measured, and the results showed that several analogs were selective σ1 receptor ligands.

Bioorganic & Medicinal Chemistry published new progress about Dopamine antagonists. 5653-62-3 belongs to class nitriles-buliding-blocks, name is 2,3-Dimethoxybenzonitrile, and the molecular formula is C9H9NO2, Name: 2,3-Dimethoxybenzonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts