38461-47-1Relevant academic research and scientific papers
A chemoselective and continuous synthesis of m-sulfamoylbenzamide analogues
Verlee, Arno,Heugebaert, Thomas,Van Der Meer, Tom,Kerchev, Pavel I.,Van Breusegem, Frank,Stevens, Christian V.
, p. 303 - 312 (2017/03/14)
For the synthesis of m-sulfamoylbenzamide analogues, small molecules which are known for their bioactivity, a chemoselective procedure has been developed starting from m-(chlorosulfonyl)benzoyl chloride. Although a chemoselective process in batch was already reported, a continuous-flow process reveals an increased selectivity at higher temperatures and without catalysts. In total, 15 analogues were synthesized, using similar conditions, with yields ranging between 65 and 99%. This is the first automated and chemoselective synthesis of m-sulfamoylbenzamide analogues.
Synthesis, docking and antidiabetic activity of some newer benzamide derivatives as potential glucokinase activators
Singh, Rohit,Lather, Viney,Pandita, Deepti,Judge, Vikramjeet,Arumugam, Karthikeyan N.,Grewal, Ajmer Singh
, p. 1 - 13 (2017/02/05)
Background: Glucokinase activators (GKAs) are the new class of candidate drugs which act on glucokinase (GK) enzyme and show their hypoglycaemic activity. Objective: The present work was planned to synthesize and evaluate the antidiabetic activity of a series of newer benzamide derivatives as potential GKAs. Method: This work involved synthesis of newer benzamide derivatives from benzoic acid and their evaluation by docking studies to determine the binding interactions for the best fit conformations in the binding site of GK enzyme. Based on the results of docking studies, the selected molecules were tested for their antidiabetic activity in the animal model. Results: Amongst the synthesized molecules, compounds 14 and 20 with phenyl-substituted thiazole moiety on amide nitrogen, exhibited highest activity in vivo. The results of the in vivo antidiabetic studies were found to be consistent with those of docking studies. Conclusion: These newly synthesized molecules thus can be treated as the initial hits for the development of new, safe, effective and orally bioavailable GKAs as therapeutic agents for the treatment of diabetic disorders.
Reactivity of 3-chlorosulfonylbenzoyl chloride in the aminolysis with aromatic amines
Tarasov,Moskvichev,Timoshenko,Frolova,Kozlova
, p. 69 - 71 (2007/10/03)
-Rate constants of the aminolysis with substituted anilines of 3-chlorosulfonylbenzoyl chloride at both chloroformyl and chlorosulfonyl groups were determined in acetonitrile at 25°C. Depending on the amine basicity, the reactivity of the chloroformyl gro
