Several new D,L beta-aminomethyl derivatives of gamma-(p-chlorophenyl)-tetrahydrofuran-2-one have been synthesized. The derivatives of D,L beta-aminomethyl-beta-(p-chlorobenzoyl)-propionic acid 2-6 were used as the substrates. These compounds were obtained by the Mannich reaction from acid 1, cyclic secondary amines and formaldehyde. After the reduction with NaBH4, and cyclization, derivatives 2-6 were converted into the appropriate derivatives of tetrahydrofuran-2-one 9-13. Some of the obtained compounds (5, 6, 8, 11 and 12) showed depressant activity against the central nervous system.
Download full-text PDF |
Source |
---|
Kidney Int
December 1991
Department of Medicine, University of Arkansas for Medical Sciences, Little Rock.
Several studies indicate an important role of platelet activating factor (PAF) and thromboxane A2 (TXA2) in glomerular pathophysiology. However, the potential role of PAF or TXA2 in renal tubular pathophysiology has received little attention, and the presence of functional receptors for these autacoids in renal tubular epithelium has not been previously studied. We examined the effects of PAF and the TXA2 analogue, ONO11113, on the cytosolic free calcium concentration [( Ca2+]i) in cultured LLC-PK1 cell line using a fluorescent probe, fura-2.
View Article and Find Full Text PDFThe synthesis of beta-aminomethyl-beta-benzoylpropionic acids (V) and beta-aminomethyl-gamma phenylbutyrolactones (VI) is described. The cis stereochemistry of compounds VI was unambiguously established by NOE experiments carried out with Vla. Antibacterial activity was studied; MIC of each derivate was determined by agar dilution in Muller-Hinton medium and application of Steers' replicator.
View Article and Find Full Text PDFArch Immunol Ther Exp (Warsz)
March 1985
Several new derivatives of 5-aminomethyl-6-/p-chlorophenyl/-4, 5-dihydro-2H-pyridazin-3-one have been obtained. The substrates, beta-aminomethyl-beta-/p-chlorobenzoyl/-propionic acid derivatives 1-5, were converted by reactions with hydrazine hydrate or monosubstituted hydrazines, i.e.
View Article and Find Full Text PDFPol J Pharmacol Pharm
July 1983
Several new derivatives of beta-aminomethyl-gamma-(p-chlorophenyl)-gamma-hydroxybutyric acids have been obtained. The substrates, beta-aminomethyl derivatives of gamma-(p-chlorophenyl)-tetrahydrofuranone-2 1-4, were converted by the reactions of ammonolysis, aminolysis and hydrazinolysis into appropriate amides and hydrazides of beta-aminomethyl-gamma-(p-chlorophenyl)-gamma-hydroxybutyric acid. Compounds 10, 11, 16, 18, 19 and 20 show depressant activity on CNS, while compounds 6 and 8 demonstrate antiinflammatory action.
View Article and Find Full Text PDFPol J Pharmacol Pharm
July 1983
Several new D,L beta-aminomethyl derivatives of gamma-(p-chlorophenyl)-tetrahydrofuran-2-one have been synthesized. The derivatives of D,L beta-aminomethyl-beta-(p-chlorobenzoyl)-propionic acid 2-6 were used as the substrates. These compounds were obtained by the Mannich reaction from acid 1, cyclic secondary amines and formaldehyde.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!