Design, synthesis and biological evaluation of new 3,4-dihydroquinoxalin-2(1H)-one derivatives as soluble guanylyl cyclase (sGC) activators

• Published in: Heliyon Vol. 8; no. 11; p. e11438
• Main Authors: Kintos, Dionysios-Panagiotis, Salagiannis, Konstantinos, Vazoura, Vasiliki, Wittrien, Theresa, Papakyriakou, Athanasios, Nikolaropoulos, Sotiris S., Behrends, Soenke, Topouzis, Stavros, Fousteris, Manolis A.
• Format: Journal Article
• Language: English
• Published: Elsevier Ltd 01.11.2022; Elsevier
• Subjects: 3,4-Dihydroquinoxalin-2(1H)-one; biological assessment; domain; enzyme activity; guanylate cyclase; heme; humans; mutants; Nitric oxide; nitroprusside; oxidants; prostatic neoplasms; sGC activators; smooth muscle; Soluble guanylyl cyclase; synergism; sGC activators; Nitric oxide; Soluble guanylyl cyclase; 3,4-Dihydroquinoxalin-2(1H)-one

Herein, we present the structure-based design, synthesis and biological evaluation of novel mono- and di-carboxylic 3,4-dihydroquinoxalin-2(1H)-one derivatives as potential heme-independent activators of soluble guanylate cyclase (sGC). Docking calculations of several known sGC agonists by utilizing...