Category: 1208318-08-4

Sun, Xicheng published the artcileStructure-activity relationship of pyrrole based S-nitrosoglutathione reductase inhibitors: Carboxamide modification, Quality Control of 1208318-08-4, the main research area is pyrrole derivative preparation nitrosoglutathione reductase inhibitor.

The enzyme S-nitrosoglutathione reductase (GSNOR) is a member of the alc. dehydrogenase family (ADH) that regulates the levels of S-nitrosothiols (SNOs) through catabolism of S-nitrosoglutathione (GSNO). GSNO and SNOs are implicated in the pathogenesis of many diseases including those in respiratory, gastrointestinal, and cardiovascular systems. The pyrrole based N6022 was recently identified as a potent, selective, reversible, and efficacious GSNOR inhibitor which is currently in clin. development for acute asthma. We describe here the synthesis and structure-activity relationships (SAR) of novel pyrrole based analogs of N6022 focusing on carboxamide modifications on the pendant N-Ph moiety. We have identified potent and novel GSNOR inhibitors that demonstrate efficacy in an ovalbumin (OVA) induced asthma model in mice.

Bioorganic & Medicinal Chemistry Letters published new progress about Asthma. 1208318-08-4 belongs to class bromides-buliding-blocks, name is Ethyl 7-(4-bromophenyl)-4,7-dioxoheptanoate, and the molecular formula is C15H17BrO4, Quality Control of 1208318-08-4.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Sun, Xicheng published the artcileDiscovery of S-Nitrosoglutathione Reductase Inhibitors: Potential Agents for the Treatment of Asthma and Other Inflammatory Diseases, HPLC of Formula: 1208318-08-4, the main research area is nitrosoglutathione reductase inhibitor preparation asthma inflammation; GSNO; GSNOR; N6022; asthma; nitric oxide; pyrrole.

S-Nitrosoglutathione reductase (GSNOR) regulates S-nitrosothiols (SNOs) and nitric oxide (NO) in vivo through catabolism of S-nitrosoglutathione (GSNO). GSNOR and the anti-inflammatory and smooth muscle relaxant activities of SNOs, GSNO, and NO play significant roles in pulmonary, cardiovascular, and gastrointestinal function. In GSNOR knockout mice, basal airway tone is reduced and the response to challenge with bronchoconstrictors or airway allergens is attenuated. Consequently, GSNOR has emerged as an attractive therapeutic target for several clin. important human diseases. As such, small mol. inhibitors of GSNOR were developed. These GSNOR inhibitors were potent, selective, and efficacious in animal models of inflammatory disease characterized by reduced levels of GSNO and bioavailable NO. N6022, a potent and reversible GSNOR inhibitor, reduced bronchoconstriction and pulmonary inflammation in a mouse model of asthma and demonstrated an acceptable safety profile. N6022 is currently in clin. development as a potential agent for the treatment of acute asthma.

ACS Medicinal Chemistry Letters published new progress about Anti-inflammatory agents. 1208318-08-4 belongs to class bromides-buliding-blocks, name is Ethyl 7-(4-bromophenyl)-4,7-dioxoheptanoate, and the molecular formula is C15H17BrO4, HPLC of Formula: 1208318-08-4.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

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