Product Details of 16629-19-9In 2022 ,《Click inspired novel pyrazole-triazole-persulfonimide & pyrazole-triazole-aryl derivatives; Design, synthesis, DPP-4 inhibitor with potential anti-diabetic agents》 appeared in Bioorganic Chemistry. The author of the article were Nidhar, Manisha; Khanam, Shaziya; Sonker, Priyanka; Gupta, Priya; Mahapatra, Archisman; Patil, Swaraj; Yadav, Brijesh Kumar; Singh, Rahul Kumar; Kumar Tewari, Ashish. The article conveys some information:
This work presented the first report on designing, synthesizing of novel pyrazole-triazole-persulfonimide and pyrazole-triazole-aryl derivatives via click reaction using CuI catalyst and evaluated for their anti-diabetic activity and DPP-4 inhibitory effect. Click reactions went smoothly with CuI catalyst in the presence of tridentate chelating ligands and produced copper-free target pyrazole-triazole-persulfonimide analogs in excellent yield at RT. The designed compounds were docked against DPP-4 enzyme and showed excellent interaction with active amino acids residue. Further, all novel pyrazole-triazole-persulfonimide and pyrazole-triazole derivatives were subjected to enzyme-based in vitro DPP-4 inhibitory activity. Based on the SAR study DPP-4 inhibitory capacity compounds 6N-((1-(3-((1,3-diphenyl-1H-pyrazol-5-yl)oxy)propyl)-1H-1,2,3-triazol-4-yl)methyl)4-methyl-N-(3-nitrobenzyl)benzenesulfonamide (9.52 nM) and 8h (4.54 nM) possessed the significant inhibition of DPP-4. Finally compounds 6N-((1-(3-((1,3-diphenyl-1H-pyrazol-5-yl)oxy)propyl)-1H-1,2,3-triazol-4-yl)methyl)4-methyl-N-(3-nitrobenzyl)benzenesulfonamide and (3-((3-methyl-1-phenyl-1H-pyrazol-5-yl)oxy)propyl)-4-(thiophen-3-yl)-1H-1,2,3triazole were evaluated for their in vivo anti-diabetic activity using STZ induced diabetic mice model, and 8h showed a significant diabetic control effect compared to the sitagliptin drug. These studies demonstrated that the novel pyrazole-triazole-persulfonimide and pyrazole-triazole-aryl derivatives might be used as the leading compounds to develop novel DPP-4 inhibitors as potential anti-diabetic agents. The results came from multiple reactions, including the reaction of Thiophene-2-sulfonyl chloride(cas: 16629-19-9Product Details of 16629-19-9)
Thiophene-2-sulfonyl chloride(cas: 16629-19-9) is a member of sulfonyl chlorides. Sulfonyl chlorides are reactive sulfonic acid derivatives similar in properties and reactivity to acid chlorides of carboxylates. The sulfonic acid group, however, is a highly hindered molecule, containing a tetrahedral configuration of substituents. Product Details of 16629-19-9
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics