309285-78-7Relevant academic research and scientific papers
Aqueous, One-Pot, Three-Component Reaction for Efficient Synthesis of 2-[4-(Arylsulfonyl)piperazin-1-yl]-1,3-benzothiazole, -1 H -benzimidazole, or -1,3-benzoxazole Derivatives
Dileep, Kommula,Murty
supporting information, p. 2295 - 2298 (2017/10/06)
A simple and efficient synthetic protocol has been developed involving a one-pot three-component reaction of a 2-chlorobenzazole, piperazine, and an arenesulfonyl chloride under aqueous conditions at room temperature in the absence of a catalyst, ligand, or base. By using this protocol, a variety of 2-[4-(arylsulfonyl)piperazin-1-yl]-1,3-benzothiazole, -1 H -benzimidazole, and -1,3-benzoxazole derivatives were synthesized in excellent yields.
Synthesis and biological analysis of benzazol-2-yl piperazine sulfonamides as 11β-hydroxysteroid dehydrogenase 1 inhibitors
Hofer, Sandra,Kratschmar, Denise V.,Schernthanner, Brigitte,Vuorinen, Anna,Schuster, Daniela,Odermatt, Alex,Easmon, Johnny
, p. 5397 - 5400 (2013/09/23)
In the last decade the inhibition of the enzyme 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) emerged as a promising new strategy to treat diabetes and several metabolic syndrome phenotypes. Using a molecular modeling approach and classical bioisosteric studies, we discovered a new class of 11β-HSD1 inhibitors bearing an arylsulfonylpiperazine scaffold. Optimization of the initial lead resulted in compound 11 that selectively inhibits 11β-HSD1 (IC50 = 0.7 μM).
