Sun, Xicheng published the artcileDiscovery of potent and novel S-nitrosoglutathione reductase inhibitors devoid of cytochrome P450 activities, Application of Ethyl 7-(4-bromophenyl)-4,7-dioxoheptanoate, the main research area is SAR preparation pyrrole S nitrosoglutathione reductase inhibitor.
The pyrrole based N6022, e.g. I, was recently identified as a potent, selective, reversible, and efficacious S-nitrosoglutathione reductase (GSNOR) inhibitor and is currently undergoing clin. development for the treatment of acute asthma. GSNOR is a member of the alc. dehydrogenase family (ADH) and regulates the levels of S-nitrosothiols (SNOs) through catabolism of S-nitrosoglutathione (GSNO). Reduced levels of GSNO, as well as other nitrosothiols (SNOs), have been implicated in the pathogenesis of many diseases including those of the respiratory, cardiovascular, and gastrointestinal systems. Preservation of endogenous SNOs through GSNOR inhibition presents a novel therapeutic approach with broad applicability. We describe here the synthesis and structure-activity relationships (SAR) of novel pyrrole based analogs of N6022 focusing on removal of cytochrome P 450 inhibition activities. We identified potent and novel GSNOR inhibitors having reduced CYP inhibition activities and demonstrated efficacy in a mouse ovalbumin (OVA) model of asthma.
Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship. 1208318-08-4 belongs to class bromides-buliding-blocks, name is Ethyl 7-(4-bromophenyl)-4,7-dioxoheptanoate, and the molecular formula is C15H17BrO4, Application of Ethyl 7-(4-bromophenyl)-4,7-dioxoheptanoate.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary