Banna N. Synthesis, physical-chemical and pharmacological properties of the gama-(R-phenyloxami-do)- and gama-(R-phenylsulfooxamido)-butanoic acids derivatives

The target-directed synthesis of the potential diuretic, anti-inflammatory, analgesic, neuroleptic and anticonvulsive action among the ?-(R-benze-neoxamido)- and ?-(R-benzenesulfooxamido)-butanoic acids has been carried out. The preparative methods by the synthesis of the new groups of biologically active compounds were developed: derivatives of ?-(R-benzeneoxamido)-butanoic acids, 2-[?-(R-benzeneoxamido)-propyl]-benzimidazoles, ?-(R-benzenesulfooxamido)-butanoic acids, ?-(4-N-R-sulfamidobenzeneoxamido)-butanoic acids, ?-(4-N-R-oxamidosulfonylbenzeneoxamido)-butanoic acids. The structure of the compounds synthesized have been confirmed by the data of the elemental analysis, UV-, IR- and NMR-spectroscopy, their purity and individuality was determined by thin-layer chromatography (TLC). Pharmacological activity of the substances synthesized has been prognosed with the PASS-program. The pharmacological screening showed the number of perspective diuretic, anti-inflammatory, analgesic, neuroleptic and anticonvulsive action. For the most active one – ?-(4-metoxycarbonylaminobenzenesul-fooxamido)-butanoic acid has been recommended for preclinical biological researches as potential preparation with anticonvulsive action.