13908-39-9Relevant articles and documents
Design, synthesis, and screening of sulfonylurea-derived NLRP3 inflammasome inhibitors
Kulkarni, Amol A.,Sajith, Ayyiliath M.,Duarte, Trevor T.,Tena, Anahis,Spencer, Charles T.,Bowen, J. Phillip
, p. 126 - 135 (2020)
Inflammasomes are multiprotein assemblies that produce robust inflammatory responses upon stimulation with pathogen- and/or danger-associated molecular patterns. Uncontrolled inflammasome activation has been linked to the pathophysiology of a wide array of disorders including life-threatening pathogenic infections, e.g., Francisella tularensis. There has been a great deal of interest in the development of small molecule inflammasome inhibitors. Using computational modeling based on chalcone derivatives, we have developed novel tertiary sulfonylurea compounds as inhibitors of the NLRP3 inflammasome. The polar enone functional alert of chalcone was replaced with a sulfonylurea scaffold while maintaining the relative positions of the two aromatic rings. These compounds were evaluated for their ability to inhibit NLRP3 and AIM2 inflammasome activation triggered by Francisella tularensis infection.
Design, synthesis, and biological evaluation of inhibitors of the NADPH oxidase, Nox4
Xu, Qian,Kulkarni, Amol A.,Sajith, Ayyiliath M.,Hussein, Dilbi,Brown, David,Güner, Osman F.,Reddy, M. Damoder,Watkins, E. Blake,Lassègue, Bernard,Griendling, Kathy K.,Bowen, J. Phillip
, p. 989 - 998 (2018/02/19)
NADPH oxidases (Nox enzymes) are critical mediators of both physiologic and pathophysiologic processes. Nox enzymes catalyze NADPH-dependent generation of reactive oxygen species (ROS), including superoxide and hydrogen peroxide. Until recently, Nox4 was proposed to be involved exclusively in normal physiologic functions. Compelling evidence, however, suggests that Nox4 plays a critical role in fibrosis, as well as a host of pathologies and diseases. These considerations led to a search for novel, small molecule inhibitors of this important enzyme. Ultimately, a series of novel tertiary sulfonylureas (23–25) was designed using pharmacophore modeling, synthesized, and evaluated for inhibition of Nox4-dependent signaling.
UREIDO SUBSTITUTED BENZOIC ACID COMPOUNDS AND THEIR USE FOR NONSENSE SUPPRESSION AND THE TREATMENT OF DISEASE
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Page 103-104, (2010/02/06)
The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.