14133-24-5Relevant academic research and scientific papers
Synthesis and anticonvulsant evaluation of some new 2-substituted-3- arylpyrido[2,3-d]pyrimidinones
White, David C.,Greenwood, Thomas D.,Downey, Aaron L.,Bloomquist, Jeffrey R.,Wolfe, James F.
, p. 5711 - 5717 (2007/10/03)
A series of 2-substituted-3-arylpyrido[2,3-d]pyrimidinones was prepared for evaluation as potential anticonvulsants. In murine screening, compounds 4a-c having a 2-oxo-2-(4-pyridyl)ethyl group in the 2-position and a 2-substituted phenyl moiety at the 3-position of the pyridopyrimidinone system displayed the most potent anti-seizure activity in both the maximal electroshock (MES) and pentylenetetrazol (scPTZ) tests at doses in the 3-10 mg/kg range. Compound 4c showed no agonist activity at the GABAA receptor and was unable to block presynaptic sodium and calcium channels in vitro.
Reactions with 2-Aminonicotinic Acid, I Some 8-Aza Analogs of Quinazolinones and Derived Tricyclic Compounds
Kassem, M. Gabr,Soliman, Farid S. G.
, p. 1197 - 1204 (2007/10/02)
The fusion of 2-acetamidonicotinic acid with o-toluidine, p-bromoaniline or o-chloroaniline afforded the corresponding 3-aryl-2-methyl-pyridopyrimidin-4(3H)-ones (4), the 8-aza analogs of 3-aryl-2-methyl-4-quinazolinones, alongside 2-aminonicotinic acid. 2-Methyl-3-(2-methylphenyl)-pyridopyrimidin-4(3H)-one (4a), the 8-aza analog of methaqualone, was converted to the 2-substituted styryl derivatives 6 by condensation with some aromatic aldehydes and to the tricyclic system, 10-aza-5,6-dihydro-3-hydroxy-5-(2-methylphenyl)-2-substituted-1H-pyridoquinazoline-1,6-diones (8) by reaction with monosubstituted bis-2,4,6-trichlorophenyl malonates. - Keywords: 10-Aza-5,6-dihydro-3-hydroxy-5-(2-methylphenyl)-2-substituted-1H-pyridoquinazoline-1,6-diones; Bis-2,4,6-trichlorophenyl malonates; 3H-Pyridopyrimidin-4-ones
Synthesis of 3,4-dihydro-4-oxoquinazoline derivatives as potential anticonvulsants
Vaidya,Panos,Kite,Iturrian,Blanton Jr.
, p. 1422 - 1425 (2007/10/02)
Twenty-three substituted 3,4-dihydro-4-oxoquinalines or 3,4-dihydro-4-oxoazaquinazolines have been synthesized utilizing 2-amino-3-cyano-4,5-dimethylfuran and methyl acrylate as precursors for synthesis of the required substituted anthranilates. Six addit
Phosphorus Pentoxide in Organic Synthesis, III. - A New Synthesis of Pyrido-pyrimidin-4(3H)-ones
Andresen, Ole R.,Pedersen, Erik B.
, p. 1012 - 1015 (2007/10/02)
Ethyl 2-acylamino-3-pyridinecarboxylates 1 were reacted with primary amine hydrochlorides, P2O5 and DMCA (N,N-dimethylcyclohexylamine) to yield a series of pyridopyrimidine-4(3H)-ones 2.The compounds 1 were prepared by acylating the corresponding e
On derivatives of 4-oxo-3,4-dihydropyrido[2,3-d]pyrimidine (author's transl)
Kretzschmar
, p. 253 - 256 (2007/10/02)
A typical representative of the hypnotic and anticonvulsive 4-quinazoline group is methaqualone (1). A number of new derivatives of 4-oxo-3,4-dihydropyrido[2,3-d]pyrimidine (10) were synthetized by substituting the benzene ring in the quinazolone molecule by the pyridine ring. The synthesis was achieved by the condensation of 2-acetaminonicotinic acid (9) and a primary amine or by the reaction of 2-aminonicotinic acid (8) with acetic acid and a primary amine. These new compounds were tested on animals for antiphlogistic, analgetic and antipyretic activities and for effects on the central nervous system as well. It was tried to establish, on the basis of the results obtained, relations between the chemical constitution and the pharmacological efficacy. It was found that, depending on the nature of the substituents in the position 3; either the antiphlogistic, analgetic and antipyretic effects or the anticonvulsive action will prevail.
