A series of substituted N-benzyl-3-chloropyrazine-2-carboxamides were prepared as positional isomers of 5-chloro and 6-chloro derivatives, prepared previously. During the aminolysis of the acyl chloride, the simultaneous substitution of chlorine with benzylamino moiety gave rise to N-benzyl-3-(benzylamino)pyrazine-2-carboxamides as side products, in some cases. Although not initially planned, t...

4-Hydroxy-2-methyl-N-(2-thiazole)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide (EX15) as nonsteroidal antiinflammatory drug (NSAIDs) of oxicam family has been synthesized bearing high selectivity for cyclooxygenase-2 (COX-2) inhibition and high ability to chelate with Cu(II) ions. The EX15Cu(II) complex, and [Cu(EX15)(OAc)(H2O)2], were synthesized and characterized by using elemental analysis...

Recent data indicated that the CB(2) cannabinoid receptor constitutes an attractive drug target due to its potential functional role in several physiological and pathological processes. A set of 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives, characterized by the presence of some important structural requirements exhibited by other classes of cannabinoid ligands, such as an aliphatic or a...

In the title compounds, N-(5-acetyl-2-methyl-phen-yl)quinoline-2-carboxamide [C19H16N2O2, (I)], N-(5-acetyl-2-bromo-phen-yl)quinoline-2-carboxamide [C18H13BrN2O2, (II)] and N-(5-acetyl-2-ethynylphen-yl)quinoline-2-carboxamide [C20H14N2O2, (III)], the quinoline ring system is essentially planar and forms a dihedral angles of 3.68 (5) (I), 5.59 (7) (II) and 1.87 (6)° (III) with the acetyl-substit...

By being an antagonist of glutamate and other receptors, kynurenic acid serves as endogenous neuroprotectant in several pathologies the brain. Unfortunately, systemic administration is hindered by its low permeability through blood–brain barrier. One possibility to overcome this problem use analogues with similar biological activity acid, but increased We synthesized six novel aminoalkylated am...

Ethnopharmacological relevance: Dysphania ambrosioides (L.) Mosyakin & Clemants (Chenopodiaceae) is a medicinal plant known for its anxiolytic, antidepressant and anticonvulsant activities in Cameroonian folk medicine. Aim of the study: The aim this work to evaluate anxiolytic effects aqueous extracts investigate mechanism action. Materials methods: Elevated plus maze test open field were u...

densely functionalized 3-(4-chlorophenyl)-5-(3-hydroxy-4-etoxyphenyl)-4,5-dihydro-1h-pyrazole-1-carboxamide was  synthesized in an expedient manner through specification and transamidation  respectively, of ester-functionalized pyrazoles. this synthetic protocol allowed for three diversifying steps in which appendages on the pyrazole scaffold were adjusted to optimize inhibition of protein kina...