Markina A. Pharmacological research of esters of N-[2-oxoindoliniliden-3)- 2-oxyacetyl]-amino acid as a potential diuretic

The thesis presents the results of the assessment of diuretic activity of 12 new derivatives N-[2-oxoindoliniliden-3)-2-oxyacetyl]-amino acid esters. Determined the lead-compound – propyl ester of N-[(2-oxoindoliniliden-3)-2-oxya- cetyl]-valine, which was called by the conventional name «Indolinoren». For this compound was calculated the defined effective dose 29.5 mg/kg. It has been established that the compound is a relatively harmless substance. It has been shown that Indolinoren in water and salt load conditions promotes increase diuresis, increase of uric acid excretion, of excretion of ions of sodium, potassium and Na+/K+ urine ratio, decrease of blood creatinine. It has been found, under condition of aldosterone receptor blockade indolinoren increased diuresis. Under condition of dopamine receptors blockade a decrease in the diuretic effect of indolinoren was noted. It has been shown antiexudative, antihypoxic, antioxidant, and antimicrobial activities of Indolinoren. The efficacy of Indolinoren was shown on test model pathologies: hemodynamic pulmonary edema and acute kidney injury by glycerol. The obtained findings substantiate reasonability of further study of Indolinoren − (N-[(2-oxoindoliniliden-3)-2-oxyacetyl]-valine propyl ester) and prospects of its clinical development as diuretic.