This review summarizes the in vitro and in vivo medicinal chemistry investigations for piperazine and morpholine analogues. Piperazine and morpholine nucleus show a broad spectrum of pharmaceutical applications, thus, in recent years, scientists has developed various new methods for the synthesis of their derivatives. This review shows current tendency in the piperazine and morpholine analogues...

The molecular properties known to play an essential role in drug-receptor interaction of substructures models of bioactive molecules have been studied using chemical quantum calculations. 1,4-diformyl-piperazine and 1,4-dithionyl-piperazine have been used as models to probe conformational behaviors and some electronic properties of substructure of some tri-substituted piperazine showing dual an...

Male strain A mice were given 0.69-18.75 g piperazine/kg Food and 0.05-2.0 g sodium nitrite (NaN02)/liter drinking water For 20-25 weeks, and were killed 10-13 weeks later. The yield of lung adenomas was significantly greater than in untreated controls when as liHle as 0.69 9 piperazine/kg plus 1.0 9 NaNOdliter, or 6.25 9 piperazine/kg plus 0.25 9 NaN02/liter, were given. A maximum of 30.7 aden...

In the liver microsome cyanide (CN)-trapping assays, piperazine-containing compounds formed significant N-methyl piperazine CN adducts. Two pathways for the N-methyl piperazine CN adduct formation were proposed: 1) The α-carbon in the N-methyl piperazine is oxidized to form a reactive iminium ion that can react with cyanide ion; 2) N-dealkylation occurs followed by condensation with formaldehyd...

The new Mannich base VEP (N,N’-bis-(5,5’-diethyl-barbituryl-1-methyl)-piperazine), has been synthetized by condensation of veronal with formaldehyde and piperazine following a Mannich procedure. The new binuclear complex Cu2VEP(X)4·4H2O , X=ClO4where VEP stands for N,N’-bis-(5,5’-diethyl-barbituryl-1-methyl)-piperazine, were obtained by metal ligand direct synthesis. Tetrahedral geometry of the...

In the title compound, C(13)H(16)ClFN(2)O, the piperazine ring is flanked by 1-(2-fluoro-benz-yl)piperazine and adopts a chair conformation. The dihedral angle between the fluoro-phenyl ring and the four planar C atoms (r.m.s. = 0.0055 Å) of the piperazine chair is 78.27 (7)°, whereas the dihedral angle between the four planar C atoms of the piperazine chair and the ethanone plane is 55.21 (9) ...

Helminths infections are chronic illness in human being and cattle. The use of alternate drugs has been a remedial measure against the resistant strains of helminth parasites, as well as means of reducing the cost of controlling diseases caused by helminthes. Pseudocedrelakotschyi is a medicinally valuable plant and possesses various pharmacological properties. P. kotschyi has been traditionall...

In vitro affinity for vascular 5HT2 and alpha receptors was determined for several compounds (spiperone, ketanserin, mianserin, trazodone, mepiprazole, benzoctamine, m-trifluoro-methylphenylpiperazine, m-chlorophenylpiperazine, and 1-(1-naphthyl)piperazine) known to interact with serotonin receptors. All compounds competitively inhibited 5HT2 and alpha receptors with differing degrees of select...