2011-06-5Relevant articles and documents
Synthesis and structure–activity relationships of aristoyagonine derivatives as brd4 bromodomain inhibitors with x-ray co-crystal research
Jung, Kwan-Young,Kim, Yeongrin,Lee, Byung Il,Lee, Joo-Youn,Lee, Kyu Myung,Park, Chi Hoon,Park, Tae Hyun,Ryu, Seong Eon,Yoo, Minjin,Yoo, Miyoun
, (2021/06/16)
Epigenetic regulation is known to play a key role in progression of anti-cancer therapeutics. Lysine acetylation is an important mechanism in controlling gene expression. There has been increasing interest in bromodomain owing to its ability to modulate t
New hybrid pyrazole and imidazopyrazole antinflammatory agents able to reduce ROS production in different biological targets
Brullo, Chiara,Massa, Matteo,Rapetti, Federica,Alfei, Silvana,Bertolotto, Maria B.,Montecucco, Fabrizio,Signorello, Maria Grazia,Bruno, Olga
, (2020/02/22)
Several anti-inflammatory agents based on pyrazole and imidazopyrazole scaffolds and a large library of substituted catechol PDE4D inhibitors were reported by us in the recent past. To obtain new molecules potentially able to act on different targets involved in inflammation onset we designed and synthesized a series of hybrid compounds by linking pyrazole and imidazo-pyrazole scaffolds to differently decorated catechol moieties through an acylhydrazone chain. Some compounds showed antioxidant activity, inhibiting reactive oxygen species (ROS) elevation in neutrophils, and a good inhibition of phosphodiesterases type 4D and, particularly, type 4B, the isoform most involved in inflammation. In addition, most compounds inhibited ROS production also in platelets, confirming their ability to exert an antiinflammatory response by two independent mechanism. Structure–activity relationship (SAR) analyses evidenced that both heterocyclic scaffolds (pyrazole and imidazopyrazole) and the substituted catechol moiety were determinant for the pharmacodynamic properties, even if hybrid molecules bearing to the pyrazole series were more active than the imidazopyrazole ones. In addition, the pivotal role of the catechol substituents has been analyzed. In conclusion the hybridization approach gave a new serie of multitarget antiinflammatory compounds, characterized by a strong antioxidant activity in different biological targets.
Benzo aza compound, preparation method and use thereof
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Paragraph 0099; 0100, (2017/08/22)
Belonging to the field of pharmaceutical chemistry, the invention relates to a benzoazepine compound, a preparation method and application thereof, in particular to the benzoazepine compound, its preparation method and application in the field of treatment of nervous system diseases, especially application in the field of drug addiction related to dopamine D1 and D3 receptors. The benzoazepine compound and pharmacologically acceptable inorganic or organic salts thereof have a structure shown as formula (I). Results of drug experiments carried out by the invention show that the benzoazepine compound and its pharmacologically acceptable inorganic or organic salts have high antagonistic activity on dopamine D1 and D3, can be used as drug leads for further development of dopamine receptor antagonists with good selectivity and high activity, and can be used as potential drugs for treatment of drug addiction by dopamine D1, D3 receptor antagonists. (formula (I)).
