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
Heterocyclic compounds
-
Page/Page column 87-88, (2015/11/09)
The invention relates to compounds of Formula I: wherein Ar1, Ar2, Ar3, L1, L2, Y, Z and v are defined in the specification, and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.
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.
N-(HETEROARYL)-SULFONAMIDE DERIVATIVES USEFUL AS S100-INHIBITORS
-
Page/Page column 100, (2014/12/12)
A compound of formula (I), or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between S100A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders.
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.
Substituted-nicotinyl thiourea derivatives bearing pyrimidine moiety: Synthesis and biological evaluation
Ke, Shaoyong,Cao, Xiufang
experimental part, p. 627 - 633 (2012/04/23)
A series of substituted-nicotinyl thiourea derivatives containing pyrimidine ring were synthesized in good to excellent yield using PEG-400 as solid-liquid phase transfer catalyst under ultrasonic irradiation. The structures of all newly synthesized compounds were elucidated and confirmed by IR, 1H NMR and elemental analysis. The preliminary biological tests show that some of the target compounds present good inhibitory activities against the root and stalk of dicotyledon plants and are safe for monocotyledon plants.
MONOCYCLIC COMPOUNDS AND THEIR USE AS TRPV1 LIGANDS
-
Page/Page column 95, (2010/06/11)
The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.
HETEROCYCLIC TRPV1 RECEPTOR LIGANDS
-
Page/Page column 169-170, (2010/06/16)
The invention relates to compounds of formulae I(a)-I(d): and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formulae I(a)-I(d) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formulae I(a)-I(d) or a pharmaceutically acceptable derivative thereof.
BICYCLOHETEROARYL COMPOUNDS AND THEIR USE AS TRPV1 LIGANDS
-
Page/Page column 123, (2010/06/14)
The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.
HETEROARYLOXY QUINAZOLINE DERIVATIVE
-
Page/Page column 72, (2010/09/05)
Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).