Hypertensive disease is not by chance considered to be one of the main problems in current medicine. This is not simply a disease, but it intrinsically decreases the quality of human life. Unfortunately, it is also a factor triggering a cascade of many pathological changes in various organs and tissues and leads to a whole series of other illnesses and pathological conditions, which contribute to widespread complications and a sharp increase in mortality. In the last decade, diuretics have secured a place in the treatment of arterial hypertension and chronic heart failure. Although being not strictly antihypertensive medicines, they lead to the elimination of a large amount of liquid from the organism thus lowering arterial pressure to a physiological norm [2, 3]. Indapamide is a particularly widely used medicine amongst this pharmacological group [4][5][6][7][8][9]. Our interest in this medicine is due not only to its biological properties. Its known structure [10] is a 2-methylindoline derivative. Quite recently, compounds with a high diuretic activity and clear antihypertensive and antiedematous properties have been found amongst 1-hydroxy-3-oxo-5,6-dihydro-3H-pyrrolo[3,2,1-ij]quinoline-2-carboxamides [11] structurally based on an unsubstituted indoline. From this there arose the idea of including methylated analogs of the above mentioned pyrroloquinolines into our search for novel diuretic compounds.

Summary Introduction: There is a high interest in creating medicines, dietary supplements, cosmetics including plant extract with antioxidant activity. For understanding whether plant extract has a maximum level of antioxidant activity it is important to know the total antioxidant activity of raw material. Objective: The main goal of study was to find out the green tea leaves total antioxidant activity. Methods: The antioxidant activity was measured by potentiometric method. Total phenolic, flavonoids, catechins and hydrocinnamic acids derivatives were quantified using Folin-Ciocalteu, aluminium chloride, vanillin and sodium molibdate methods, respectively. Results: The green tea leaves total antioxidant activity was 660.75 mmol-eqv./mres. dry weight. A significant correlation was observed between the amount of phytochemicals and antioxidant activity, which indicated its main role in antioxidant activity. Conclusion: The research showed that the green rea leaves possess a high value of antioxidant activity and it is a good source of phenolic constituents.

Keywords: 4-hydroxy-2-oxoquinoline-3-carboxylic acid alkylamides, amidation, diuretic activity, X-ray structural analysis.The accidental discovery of stimulation of diuretic function of the kidney [2] using 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides (which had not previously been considered as a specific feature) has since then proved to be a trigger for carrying out a broad investigation targeted towards a novel class of diuretic chemicals. As a result, compounds have been synthesized which (due to the mechanism of the removal of a large volume of liquid [3]) have proved efficient agents in the fight against serious pathology such as hypertensive disease and also edema in the brain and lungs [4].With the aim of discovering novel compounds which would be of interest as the basis for preparing therapeutically useful diuretic materials, one of the directions of our further work related to the 1-hydroxy-3-oxo-6,7-dihydro-3H,5H-pyrido[3,2,1-ij]quinoline-2-carboxylic acid N-R-amides 1. A justification for studying such substances is their close structural similarity to 1-hydroxy-3-oxo-5,6-dihydro-3H-pyrrolo-[3,2,1-ij]quinoline-2-carboxamides [4,5] which have high diuretic activity. Expansion of the ring annelated to the quinolone nucleus by just one unit should certainly lead to a conformational rearrangement of of the basic molecule and this, in turn, can bring about changes in pharmacological properties.In principle, the synthesis of the starting ethyl 1-hydroxy-3-oxo-6,7-dihydro-3H,5H-pyrido[3,2,1-ij]-quinoline-2-carboxylate (2) can be achieved by the reaction of 1,2,3,4-tetrahydroquinoline (3) with triethylmethane tricarboxylate (4) using different methods, i.e. holding a mixture of the amine and a twofold excess of acylating agent at 220ºC [6] or by the stepwise addition of the amine to an equimolar amount of the _______ * For Communication 193, see [1].

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A comparative analysis of the effect of halo-substituted anilides of 6-hydroxy-4-oxo-2,4-dihydro-1H-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acids on the urinary function of the kidney has shown that methylation of the pyrroline ring at position 2 leads to an increased diuretic effect. As a method for improving the pharmacological properties of this class of compounds, it deserves more detailed attention [2]. The most promising substance or structural leader in the group of unmethylated derivatives was found to be the 6-hydroxy-4-oxo-2,4-dihydro-1H-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acid 4-methoxyanilide [3]. Hence it was quite logical that the next step in our study should be examination of the corresponding alkoxy-and hydroxyanilides of 6-hydroxy-2-methyl-4-oxo-2,4-dihydro-1H-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acid 1a-j. O OH O OEt N Me O OH O N N H Me R N H 2 R 1a-j 2 1a R = 2-ОH; b R = 3-ОН; c R = 4-ОН; d R = 2-ОМе; e R = 3-ОМе; f R = 4-ОМе; g R = 2-Me-4-OMe; h R = 4-OEt; i R = 4-OPr; j R = 4-OC 6 H 13