Alcohol-water extracts of Thymus vulgaris have obtained by ultrasonic extraction method for different times extraction. The obtained extracts have been tested for the quantitative content of extractive substances, phenolic compounds and flavonoids and for the presence of antioxidant activity. The best studied indicators were found in extract obtained by ultrasound extraction for 40 minutes (content of extractive substances 25 mg / ml, sum of polyphenolic compounds 30 mg / ml, flavonoids content 45 mg / ml).

The investigation is devoted to the assessment of the potential antimicrobial use of new chalcogen-functionalized thiazolo[2,3-b]quinazolin-5-ones, halides and trihalides of thiazolo[3,2-a]quinazolin-10-ium and tribromides thiazino[3,2-a]quinazolin-11-ium. The compounds under study were obtained by electrophilic intramolecular heterocyclization. A high bactericidal and fungicidal effect against some gram-positive and gram-negative bacteria and fungi has been revealed for the investigated compounds. The "structure-activity" relationship has been established; the influence of the chalcogen's nature and the type of substituents in the thiazoline and pyrimidine cycles on the biological activity of the investigated thiazolo- and thiazinoquinazolines is shown. Angular 4-methyl-5-oxo-1-((trihalogenotellanyl)methylidene)-8-(trifluoromethyl)-1,2,4,5-tetrahydrothiazolo[3,2-a]quinazolin-10-ium halides have been found to show the highest bactericidal activity to the gram-negative culture of Escherichia coli.

No abstract

Досліджено нуклеофільність аміногрупи у 2-положенні 1,4-нафтохіноїдного фрагменту порівняно з нуклеофільними властивостями аміногруп у 6-та 7-положенні в реакціях алкілювання, ацилювання, а також при взаємодії з сульфінілхлоридами та сульфонілхлоридами. Встановлено, що за наявності аміногрупи у молекулі заміщеного 1,4-нафтохінону відбувається зсув електронної густини в сторону нафтохіноїдного циклу з відповідною зміною заряду на атомах вуглецю у певному положенні. Таким чином реакційна здатність аміногрупи в реакції алкілювання найвища у 7-му атомі вуглецю, дещо нижча активність аміногрупи у 6-му положені і найнижча у 2-положенні 1,4-нафтохінону. Ключові слова: 1,4-нафтохінон, реакції алкілювання та ацилювання, сульфінілхлорид, сульфонілхлорид.

Quinoid derivatives are attractive not only as interesting synthons for synthesis, but also as potential biologically active substances, so it is important to modify the compounds of the quinone series with different pharmacoform fragments. In this work, the structural design of chlorine and bromanyl disulfur-containing fragments, namely thiosulfonate, and chloranyl – a fragment of 4- aminobutanoic acid. Methods of synthesis were developed and physicochemical characteristics of thiosulfonate and amino acid derivatives were studied: 2,5-bis (thiosulfonate) -3,6-halogen -1,4- benzoquinones and 2,5-bis (3-carboxypropylamino) -3,6 - dichlorobenzoquinone. The prospects for the design of chlorine and bromanyl thiosulfonate fragments and chloranyl fragment of 4- aminobutanoic acid are confirmed by the results of predicting the biological activity of 5 a, b, 6 a, b, 7 using the online resource PASS Online. In particular, the substance 6a obtained by us is promising in terms of research on Antiviral (Picornavirus). The obtained results of predicted cytotoxicity screening indicate the feasibility of conducting experimental studies by in vitro methods on anticancer activity against cancer cell lines of hematopoietic and lymphoid tissue, lungs, skin, ovaries, blood, breast, kidney, colon, brain.