57164-96-2Relevant academic research and scientific papers
Mild hypervalent iodine mediated oxidative nitration of N-aryl sulfonamides
Kloeckner, Ulrich,Nachtsheim, Boris J.
, p. 10485 - 10487 (2014)
An oxidative and acid-free method for the nitration of N-aryl sulfonamides has been developed using a combination of sodium nitrite as cheap and easy to handle NO2-source and the hypervalent iodine reagent PIFA as stoichiometric oxidant. Under
Lead optimization of selective tubulin inhibitors as anti-trypanosomal agents
Zhao, Anran,Li, Yaxin,Orahoske, Cody M.,Schnur, Brittny,Sabbagh, Abboud,Zhang, Wenjing,Li, Bibo,Su, Bin
, p. 1517 - 1528 (2019/03/05)
Previously synthesized tubulin inhibitors showed promising in vitro selectivity and activity against Human African Trypanosomiasis. Current aim is to improve the ligand efficiency and reduce overall hydrophobicity of the compounds, by lead optimization. V
Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template
Ann, Jihyae,Sun, Wei,Zhou, Xing,Jung, Aeran,Baek, Jisoo,Lee, Sunho,Kim, Changhoon,Yoon, Suyoung,Hong, Sunhye,Choi, Sun,Turcios, Noe A.,Herold, Brienna K.A.,Esch, Timothy E.,Lewin, Nancy E.,Abramovitz, Adelle,Pearce, Larry V.,Blumberg, Peter M.,Lee, Jeewoo
, p. 3603 - 3607 (2016/07/21)
A series of homologous analogues of prototype antagonist 1 and its urea surrogate were investigated as hTRPV1 ligands. Through one-carbon elongation in the respective pharmacophoric regions, N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea was identified as a novel and potent TRPV1 antagonistic template. Its representative compound 27 showed a potency comparable to that of lead compound 1. Docking analysis of compound 27 in our hTRPV1 homology model indicated that its binding mode was similar with that of 1S.
