Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4)

Abstract

Pal, Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4

Thiourea Dioxide Catalyzed Sustainable Synthesis of Diverse Quinoxaline and Pyrazine Derivatives in Aqueous Medium at Ambient Temperature

“…Interestingly, these derivatives are also found in the structure of commercially available drugs such as Quinacillin (an antibacterial drug), [3] Varenicline (a partial agonist drug used for smoking cessation), [4] Brimonidine (used to treat open‐angle glaucoma, ocular hypertension, and rosacea), [5] Panadiplon (an anxiolytic drug), [6] Morinamide (an anti‐tuberculosis agent), [7] and Glipizide (an anti‐diabetic agent) [8] (Figure 1). Another fascinating aspect of quinoxaline and pyrazine scaffolds is that when combined with other bioactive fragments, especially with indole or indene, they create compounds with a variety of pharmaceutical properties [9–11] . These fused heterocycles also possess applications in diverse technical fields, like in the production of organic semiconductors, [12] metal complexes, [13] cavitands, [14] dyes, [15] luminescent materials, [16] and more.…”

“…Another fascinating aspect of quinoxaline and pyrazine scaffolds is that when combined with other bioactive fragments, especially with indole or indene, they create compounds with a variety of pharmaceutical properties. [9][10][11] These fused heterocycles also possess applications in diverse technical fields, like in the production of organic semiconductors, [12] metal complexes, [13] cavitands, [14] dyes, [15] luminescent materials, [16] and more.…”

Microwave Assisted Synthesis of 3-Chloro-N-(2-(5-chloro-1-tosyl-1Hbenzo [d] Imidazol-2-yl) ethyl)-N-Substituted Quinoxalin-2-Amine Derivatives Using DCQX

“…This method is facilitated by AlCl 3 on forming C-N bond [1] . These target molecules were found to be potential inhibitors of phospho diesterase 4 (PDE-4) and have apoptosis inducing properties in an animal model (zebrafish) [12,13] . Further, the reaction is facilitated in more effective way using an alkylating agent, propargyl bromide.…”