1422166-44-6Relevant academic research and scientific papers
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)
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.
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 (2019/11/25)
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.
NADPH OXIDASE INHIBITORS AND USES THEREOF
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Page/Page column 5; 55, (2019/02/13)
This disclosure relates to compounds and methods of treating or preventing a Nox related disease or condition comprising administering to a subject in need thereof a Nox inhibitor or pharmaceutical compositions comprising a Nox inhibitor disclosed herein,
Synthesis and structure-activity relationship studies of novel dual inhibitors of soluble epoxide hydrolase and 5-lipoxygenase
Meirer, Karin,R?dl, Carmen B.,Wisniewska, Joanna M.,George, Sven,H?fner, Ann-Kathrin,Buscató, Estella,Klingler, Franca-Maria,Hahn, Steffen,Berressem, Dirk,Wittmann, Sandra K.,Steinhilber, Dieter,Hofmann, Bettina,Proschak, Ewgenij
supporting information, p. 1777 - 1781 (2013/03/29)
Current research leads to the assumption that drugs affecting more than one target could result in a more efficient treatment of diseases and fewer safety concerns. Administration of drugs inhibiting only one branch of the arachidonic acid cascade is usua
