123565-82-2Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS IMAGING PROBES OF TAU PATHOLOGY
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Page/Page column 57, (2013/07/05)
Pyridazinone compounds of Formula I: (I) wherein: R' is alkyl or Ar, optionally substituted with at least one alkyl, halo? gen, hydroxyl, alkoxy, haloalkoxy, acid, ester, amino, nitro, amide, or alkoxyhalo; 2 R is independently alkyi, alkynyl, ester, amino, amide, acid, aryl, heteroaryl, aminoalkyl, -C(=0)alkyl, -C(=0)aryl, -C(=0)heteroaryl, -C(=0)heterocycloalkyl, - C(=0)heterocycloalkylAr, -C(=0)(CH2)nhalo, -C(=0)(CH2)nheterocyclyl, or -SC^Ar, optionally substituted with at least one alkyi, alkylhalo, halogen, nitro, aryl, heteroaryl, or heteroaryl(CH2)nhalo; R 3 and R4 are independently hydrogen, alkyi, alkenyl, alkynyl, aryl, heteroaryl; Ar is an aryl, heteroaryl, cycloalkyl, heterocycloalkyl group; n is an integer from 0-10; or a radiolabeled derivative thereof. The compounds are useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.
2-Aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists
Ferguson, Gemma N.,Valant, Celine,Horne, James,Figler, Heidi,Flynn, Bernard L.,Linden, Joel,Chalmers, David K.,Sexton, Patrick M.,Christopoulos, Arthur,Scammells, Peter J.
experimental part, p. 6165 - 6172 (2009/10/09)
A pharmacophore-based screen identified 32 compounds including ethyl 5-amino-3-(4-tert-butylphenyl)-4-oxo-3,4-dihydrothieno[3,4-d] pyridazine-1-carboxylate (8) as a new allosteric modulator of the adenosine A1 receptor (A1AR). On the basis of this lead, various derivatives were prepared and evaluated for activity at the human A 1AR. A number of the test compounds allosterically stabilized agonist-receptor-G protein ternary complexes in dissociation kinetic assays, but were found to be more potent as antagonists in subsequent functional assays of ERK1/2 phosphorylation. Additional experiments on the most potent antagonist, 13b, investigating A1AR-mediated [35S]GTPγS binding and [3H]CCPA equilibrium binding confirmed its antagonistic mode of action and also identified inverse agonism. This study has thus identified a new class of A1AR antagonists that can also recognize the receptor's allosteric site with lower potency.
STUDIES ON ALKYLHETEROAROMATIC COMPOUNDS: NEW SYNTHESES OF 1,3,4-OXADIAZOLE, OXADIAZOLOPYRIDINE, 1,3,4-THIADIAZOLE, THIADIAZOLOPYRIDINE, PHTHALAZINE AND THIENOPYRIDAZINE DERIVATIVES.
Elnagdi, Mohamed Hilmy,Erian, Ayman Wahba,Sadek, Kamal Usef,Selim, Maghraby Ali
, p. 1124 - 1142 (2007/10/02)
Ethyl 5-phenyl-1,3,4-oxadiazol-2-ylacetate (3a) could be prepared via condensation of ethyl 3-amino-3-ethoxyprop-2-enoate (1) with benzoylhydrazine.This product coupled with aromatic diazonium salts to yield arylhydrazones 4a,b.Compound 3a was converted i
α,β-Unsaturated Nitriles in Heterocyclic Synthesis: Synthesis of Several Arylpyridine and Arylpyridazine Derivatives
Elgemeie, Galal Hamza,Elfahham, Hassan Attia,Ibrahiem, Yusria Rizk,Elnagdi, Mohamed Hilmy
, p. 535 - 540 (2007/10/02)
Several new azabiaryls and diazabiaryls were synthesized utilizing readily obtainable α,β-unsaturated nitriles.
Studies with Alkylheteroaromatic ?-Deficient Compounds: Novel Synthesis of Thienopyridazines and Phthalazines
Elnagdi, Mohamed Hilmy,Negm, Abdalla Mohamed,Erian, Ayman Wahba
, p. 1255 - 1256 (2007/10/02)
Ethyl 1-aryl-5-cyano-1,6-dihydro-4-methyl-6-oxo-3-pyridazinecarboxylates 1 react with elemental sulphur in ethanolic basic solutions to yield thienopyridazines 2.Compounds 2 readily react with electron-deficient olefins to yield phthalazines.
