УДК: 616–093+547.789

The present microreview provides access to recent advances in the synthetic approaches to novel thiazolo[4,5-b]-pyridines developed over the last years. This second part presents the overview and analysis of modern synthetic techniques for thiazolo[4,5-b]pyridine bicyclic scaffold construction starting from pyridine derivatives followed by thiazole heterocycle annulation

УДК: 616–093+547.789

As a result of the furfural reaction with diazonium, salts 1a-h the arylfuran-2-carbaldehydes 3a-h were synthesized. In the reaction of Wilgerodt-Kindler, arylfuran-2-carbaldehydes with sulfur and aryl piperazines was prepared 1-aryl-4-[(5-aryl-2-furyl)carbonothioyl]piperazines. The structures of target compounds 5a-l were confirmed by using 1H NMR spectroscopy and elemental analysis. The antimicrobial activity of the synthesized substances was evaluated by the value of the MIC and minimum fungicidal and bactericidal concentration. The findings exhibited that the compounds
possessed moderate antimicrobial potential. In vitro anticancer activity assessment on the full panel

УДК 615.038;615.276

Метою роботи було виявити протизапальний ефект нового похідного з групи 4-тіазолідинонів — Les6490, для чого проведено порівняльне дослідження впливу двох засобів: сполуки Les6490 і німесуліду, який належить до групи нестероїдних протизапальних препаратів з вираженою протизапальною, анальгезивною та жарознижувальною дією. Німесулід зараховують до високоселективних інгібіторів циклооксигенази та її ізоферментів (ЦОГ-2) і використовують за різних патологій опорно-рухового апарату. Новосинтезована сполука Les6490 належить до групи похідних 4-тіазолідинонів. Тіазолідинонове кільце входить до складу багатьох наявних потенційних антибактеріальних та протизапальних засобів, може комбінуватись з піразоловими фрагментами, які є фармакоформами тієї ж структури, і здатне сприяти підвищенню терапевтичної ефективності. У роботі досліджено особливості змін гематологічних показників у щурів за експериментального відтворення асоційованого запального процесу за використання моделі ад’ювант Фрейнда (ПАФ). У результаті дослідження протизапальної активності за гематологічними показниками препаратів — Les6490 та німесуліду — виявлено їхню протизапальну активність, яку можна вважати співставною з незначною перевагою сполуки Les6490. При цьому, не виявляючи впливу на кількісний рівень еритроцитів за ізольованого введення, в умовах запального процесу німесулід та Les6490 спричиняли вірогідне збільшення загальної кількості еритроцитів порівняно групою з модельованим запаленням. Не виявлено жодного впливу на кількість гемоглобіну. За аналізу показників лейкоцитарної формули активність сполуки Les6490 є схожою до німесуліду. Найбільш виражені зміни лейкоцитарної формули за АФ-індукованого запалення спостерігали з боку нейтрофілів: дія досліджуванної речовини Les6490 була вираженішою порівняно з дією німесуліду. Введення сполуки Les6490 частково спричиняло нормалізацію моноцитів, а за умов АФ-асоційованого запального процесу вірогідних змін не спостерігали.
Ключові слова: німесулід, Les6490, 4-тіазолідинони, нестероїдні протизапальні препарати, еритроцити, гемоглобін, лейкоцити

The aim of the work was to identify the anti-inflammatory effect of a newly synthesized drug from the group of 4-thiazolidinones. Thus, a comparative study of the effect of two agents was conducted: the drug Les6490 and the non-steroidal anti-inflammatory drug nimesulide. This drug belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs), which have pronounced anti-inflammatory, analgesic and antipyretic effects. Nimesulide belongs to highly selective inhibitors of cyclooxygenase and its isoenzymes (COX-2) and is used for treatment in various pathologies of the musculoskeletal system. The newly synthesized compound Les6490 belongs to the group of 4-thiazolidinone derivatives. The thiazolidinone ring is part of many existing potential antibacterial and anti-inflammatory agents, and can be combined with pyrazole fragments, which are pharmacophores of the same structure, and can contribute to …

Biometric parameters of fruits and seeds of Paulownia tomentosa collected from trees growing in soil and climatic conditions of different geographical locations of Odesa, Zakarpattia (Mukachevo) and Lviv regions of Ukraine, as well as technical and absolute germination, germination energy, mean germination time and weight of 1000 seeds, were studied. The effect of different temperatures on seed germination in soil was evaluated under two temperature regimes. The influence of the duration of pre-soaking on seed germination was also determined. Pre-soaking
of seeds in water and solutions of five different stimulants on germination in soil was also investigated. It has been found that in the conditions of Odesa region, the species formed larger fruits and the seeds were characterized by significant rate and uniformity of germination. Lowering of germination temperature caused a decrease in germination energy, laboratory and absolute seed germination, and increased the mean germination time of seeds. Pre-soaking of seeds increased significantly germination rate and its duration was associated with the parameters: germination energy, technical and absolute germination. Among the three seed collections, the highest technical germination was recorded for seeds from Lviv region. The seeds from Odesa region had the highest germination energy. The seeds were characterized by high germination rate in soil regardless of the geographical location of seed collection under the conditions of Ukraine. The highest germination in soil was found for seeds, collected in Lviv. Temperature during germination significantly affected the germination of seeds in soil. Under the temperature regime of 21 to 25 °C, soil fertility parameters were significantly higher. Pre-soaking of seeds had the highest stimulating effect on further germination of seeds in soil among the studied treatments. Pre-treatment of seeds with germination stimulants had generally a positive effect, increasing germination in soil.
Key words: biometric parameters, germination, pre-soaking, stimulators, temperature regimes, weight of 1000 seeds

The forest raw material base of Ukraine needs a long-term recovery, caused by current shortage of wood and in the long-term perspective, as well. One of the ways to solve this problem is to create plantations of Paulownia tomentosa (Thunb.) Steud., which are able to accumulate in a very short time a significant stock of wood, suitable for industrial use. Determination of the physical and mechanical properties was carried out on samples of standard sizes. It has been established that the density of paulownia wood, grown under the conditions of the Western Forest Steppe of Ukraine, ranges from 329–342 kg·m-3 (sapwood, heartwood) to 416 kg·m-3 (middle part between the sapwood and heartwood). Under the conditions when only air moisture influences the wood, the moisture content increases up to 12.9 %. Static bending strength, compressive strength parallel to grain, static hardness, modulus of elasticity of sapwood and heartwood parts of the trunk are characterized by minimum values, and the middle part (between the sapwood and heartwood) – by maximum ones. Therefore, in terms of appearance and texture, the wood has the most similarity with the wood of common ash; considering its density value, paulownia wood resembles the wood of Norway spruce and silver fir, but due to lower moisture absorption and the content of tannins, it is more resistant to decay than the mentioned species; the middle part according to some mechanical indicators is close to common pine wood, therefore, it can be widely used in building industry. Paulownia tomentosa wood is advisable to be used as a promising material for the production of firewood and wood pellets. The data we have obtained can be taken into account by specialists in the woodworking, furniture and agricultural industries when planning the creation of plantations and the use of its wood.
Key words: modulus of elasticity, moisture content, plantations, porosity, shrinkage, strength,
swelling.