- November 11, 2011 - S-Nitrosoglutathione Reductase Inhibitors for the Prevention and Treatment of Experimental Colitis
- August 28, 2011 - Structure – Activity Relationships of Pyrrole Based S-Nitrosoglutathione Reductase Inhibitors – Carboxamide Modification
- July 14, 2011 - Heterozygous Deletion of S-Nitrosoglutathione Reductase in Mice Does Not Increase Nitrosative Inactivation of O6-Alkylguanine-DNA Alkyltransferase or Diethylnitrosamine-induced Hepatocarcinogenesis
- May 3, 2011 - Oral S-Nitrosoglutathione Reductase Inhibitors Attenuate Pulmonary Inflammation and Decrease Airspace Enlargement in Experimental Models of COPD
- March 27, 2011 - Discovery of S-nitrosoglutathione reductase inhibitors as potential agents to treat asthma, COPD and IBD
More posters
|
April 19, 2011 Structure–activity relationships of pyrrole based S-nitrosoglutathione reductase inhibitors: Pyrrole regioisomers and propionic acid replacement
Xicheng Sun, Jian Qiu, Sarah A. Strong, Louis S. Green, Jan W.F. Wasley, Joan P. Blonder, Dorothy B. Colagiovanni, Sarah C. Mutka, Adam M. Stout, Jane P. Richards, Lawrence Chun, Gary J. Rosenthal
S-Nitrosoglutathione reductase (GSNOR) is a member of the alcohol 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, cardiovascular, and gastrointestinal systems. The pyrrole based N6022 was recently identified as a potent, selective, reversible, and efficacious GSNOR inhibitor which is currently undergoing clinical development.
We describe here the synthesis and structure–activity relationships (SAR) of novel pyrrole based analogues of N6022 focusing on scaffold modification and propionic acid replacement. We identified equally potent and novel GSNOR inhibitors having pyrrole regioisomers as scaffolds using a structure based approach.
Bioorganic & Medicinal Chemistry Letters 21 (2011) 3671–3675. (More…Science Direct website) 
Comments are closed.
|
- January 24, 2013 - Pharmacological Inhibition of S-Nitrosoglutathione Reductase Improves Endothelial Vasodilatory Function in Rats in vivo
- December 28, 2012 - ADH IB Expression, but Not ADH III, Is Decreased in Human Lung Cancer
- February 15, 2012 - Mechanism of Inhibition for N6022, a First-in-Class Drug Targeting GSNOR
- January 13, 2012 - Structure–activity relationship of pyrrole based GSNOR inhibitors
- August 25, 2011 - Preclinical 28-Day Inhalation Toxicity Assessment of S-Nitrosoglutathione
- July 26, 2011 - Discovery of potent and novel GSNOR inhibitors devoid of cytochrome P450 activities
- April 19, 2011 - Structure–activity relationships of pyrrole based GSNOR inhibitors: Pyrrole regioisomers and propionic acid replacement
|
