600162-05-8Relevant academic research and scientific papers
Identification of arylsulfonamides as ExoU inhibitors
Kim, Doran,Baek, Jihae,Song, Jiho,Byeon, Hyeyoung,Min, Hyeyoung,Min, Kyung Hoon
, p. 3823 - 3825 (2014)
ExoU is a potent virulence factor of Pseudomonas aeruginosa and is considered a potential therapeutic target. In order to discover novel ExoU inhibitors, we screened an in-house chemical library utilizing a yeast-based screening system. Some sulfonamides displayed significant activity without nonspecific cytotoxicity. We describe a series of sulfonamides as novel ExoU inhibitors, along with a brief structure-activity relationship.
Synthesis, characterization and biological screening of some new sulfonamides derivatives of 1,4-benzodioxane-6-amine
Irshad, Misbah,Abbasi, Muhammad Athar,Rehman, Aziz-Ur,Siddiqui, Sabahat Zahra,Ashraf, Muhammad,Ejaz, Syeda Abida,Lodhi, Muhammad Arif,Jamal, Syed Babar
, p. 660 - 673 (2014/12/11)
In the present study, a series of N-substituted derivatives of 1,4-benzodioxane-6-amine have been synthesized. The reaction of 1,4-benzodioxane-6-amine (1) with various alkyl/aryl sulfonyl chlorides (2a-k) yielded N-alkyl/aryl sulfonamides (3a-k), which further on treatment with benzyl chloride (4) in the presence of sodium hydride furnished into N-benzylated sulfonamides (6a-k) while the reaction of 3a-k with ethyl iodide (5 ) yielded N-ethylated sulfonamides 7a-k. These derivatives were characterized by IR, 1H-NMR and EI-MS and then screened against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and lipoxygenase (LOX) enzymes and were found to be good inhibitors of lipoxygenase only. The interaction between inhibitors and target enzymes were computationally observed which correlates with the experimental results.
