54127-29-6Relevant articles and documents
Rational design of a fluopyram hapten and preparation of bioconjugates and antibodies for immunoanalysis
Ceballos-Alcantarilla,Agulló,Abad-Fuentes,Abad-Somovilla,Mercader
, p. 51337 - 51341 (2015/06/25)
A fluopyram hapten was designed in which insignificant electronic and structural modifications were foreseen and all potentially interacting chemical moieties were maintained. This hapten was prepared by total synthesis and three immunologically active bi
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket
Hong, Fang-Tsao,Norman, Mark H.,Ashton, Kate S.,Bartberger, Michael D.,Chen, Jie,Chmait, Samer,Cupples, Rod,Fotsch, Christopher,Jordan, Steven R.,Lloyd, David J.,Sivits, Glenn,Tadesse, Seifu,Hale, Clarence,St. Jean, David J.
, p. 5949 - 5964 (2014/08/18)
Structure-activity relationship investigations conducted at the 5-position of the N-pyridine ring of a series of N-arylsulfonyl-N′-2-pyridinyl- piperazines led to the identification of a novel bis-pyridinyl piperazine sulfonamide (51) that was a potent disruptor of the glucokinase-glucokinase regulatory protein (GK-GKRP) interaction. Analysis of the X-ray cocrystal of compound 51 bound to hGKRP revealed that the 3-pyridine ring moiety occupied a previously unexplored binding pocket within the protein. Key features of this new binding mode included forming favorable contacts with the top face of the Ala27-Val28-Pro29 ("shelf region") as well as an edge-to-face interaction with the Tyr24 side chain. Compound 51 was potent in both biochemical and cellular assays (IC50 = 0.005 μM and EC 50 = 0.205 μM, respectively) and exhibited acceptable pharmacokinetic properties for in vivo evaluation. When administered to db/db mice (100 mg/kg, po), compound 51 demonstrated a robust pharmacodynamic effect and significantly reduced blood glucose levels up to 6 h postdose.
4-Azolylphenyl isoxazoline insecticides acting at the GABA gated chloride channel
Lahm, George P.,Cordova, Daniel,Barry, James D.,Pahutski, Thomas F.,Smith, Ben K.,Long, Jeffrey K.,Benner, Eric A.,Holyoke, Caleb W.,Joraski, Kathleen,Xu, Ming,Schroeder, Mark E.,Wagerle, Ty,Mahaffey, Michael J.,Smith, Rejane M.,Tong, My-Hahn
, p. 3001 - 3006 (2013/06/26)
Isoxazoline insecticides have been shown to be potent blockers of insect GABA receptors with excellent activity on a broad pest range, including Lepidoptera and Hemiptera. Herein we report on the synthesis, biological activity and mode-of-action for a class of 4-heterocyclic aryl isoxazoline insecticides.