ACTOPROTECTOR ACTIVITY OF 4-R-(IDENEAMINO)- 5-R-4Н-1,2,4-TRIAZOLE-3-THIOLS

In this study, actoprotector activity of 1,2,4-triazole derivatives is described. The biological activity of synthetic 4-R-(ideneamino)-5-R-4Н-1,2,4-triazole-3- thiols was analyzed. The forced swim test with a weight load of 10% of the test animal’s body weight was applied. According to the obtained results, compounds that contained NH4+ and CuSO4 substituents were among the most active, potency of which was close to that of the reference drug Riboxin. Introduction of propylamine, isopropylamine and piperazine groups into the molecule decreases the actoprotector activity. Compounds containing monoethanolamine, diethylamine, ethylamine, and magnesium sulfate moieties almost did not exhibit actoprotector activity.In this study, actoprotector activity of 1,2,4-triazole derivatives is described. The biological activity of synthetic 4-R-(ideneamino)-5-R-4Н-1,2,4-triazole-3- thiols was analyzed. The forced swim test with a weight load of 10% of the test animal’s body weight was applied. According to the obtained results, compounds that contained NH4+ and CuSO4 substituents were among the most active, potency of which was close to that of the reference drug Riboxin. Introduction of propylamine, isopropylamine and piperazine groups into the molecule decreases the actoprotector activity. Compounds containing monoethanolamine, diethylamine, ethylamine, and magnesium sulfate moieties almost did not exhibit actoprotector activity

Synthesis and properties of bis((4-R-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)alkanes

The aim of this work was the synthesis of bis((4-R-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)alkanes using available reagents and study of their properties. Matherial and methods. 4-R-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-thiol was used as an intermediate compound, obtained from methyl 2-(thiophen-2-yl)acetate. Its synthesis has been described in previous studies. During the bis((4-R-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)alkane moiety formation stage, dibromoalkanes (dibromomethane, dibromopropane, dibromobuthane) were used as secondary reagents. The reaction was conducted in propan-2-ol. The presence of reaction products has been confirmed applying spectral methods. Synthesis of bis((4-R-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)alkanes 0.01 M of the correspondent alkyl halide is added to the corresponding 3-(3-R-1,2,4-triazol-5-thiomethyl)-1,2,4-triazol-5-thione (0.01 M) in mixture of 0.01 mole NaОН and 30 mL of ethanol or propan-1-ol, and the mixture is boiled until the neutralization (during 3 hours reflux). The mixture is filtered, solvent is evaporated. White crystalline matter, practically insoluble in water, soluble in organic solvents. Compounds were purified by recrystallization from dimethylformamide-water mixture (1:1). Results. Distinction of compounds was confirmed by chromatography-mass-spectrometry. 1H NMR spectra of the obtained compounds were characterized by number of signals. The protons of alkylsulfide fragment resonate in a weak field appearing as multiplets at 3.12–3.07 ppm and 2.25–2.10 ppm. The protons of methyl group, which bond the heteroaromatic fragments together, resonate as a singlet at 3.92–3.87 ppm. Aromatic protons of thiophene fragments appear as multiplets at 6.95–6.78 and 6.99–7.20 ppm. The protons of methyl fragment of N-alkyl substituent appear as a multiplet at 4.21–3.98 ppm, protons of methyl fragment resonate as a triplet at 1.52–1.57 ppm. IR spectra of the studied compounds showed presence of C-S fragment, which appears as a band of molecular stretching at 693 cm-1. Stretching vibrations of С-H fragment of thiophene ring is observed at 715–693 cm-1. The CH2 fragment appears as strong stretching (at 2935–2905 cm-1 and 2865–2855 cm-1) and moderate bending vibrations (at 1493–1460 cm-1). Also recommended for “polymethylene fragment” are characteristic deformation vibrations at 730–720 cm-1. Symmetrical and asymmetrical bending at 1385–1380 and 1470–1465 cm-1characterize the presence of СН3 group. Preliminary screening of acute toxicity and biological activity parameters has been carried out. Conclusions. Nine compounds were obtained; their structures were confirmed.The characteristics of the synthesized compounds were assessed with computer processing using PASS online tool. The most promising compounds were selected for in vitro research. It was clarified during the analysis of results that the obtained compounds may exhibit various types of biological activities. The most probable effect predicted for the nine studied compounds is antimicrobial activity. 1,2,4-triazole, bis-derivatives, synthesis, IR spectroscopy, 1Н NMR spectroscopy, PASS-screenin

Вивчення антиоксидантної активності солей 2-((4-R-3-(морфолінометилен)-4H-1,2,4-тріазол-5-іл)тіо)ацетатних кислот

In this work we have conducted the synthesis, the establishment of physical-chemical properties and subsequent Pass-screening of possible biological activity for new alkyl derivatives of 4-R-3-(morfolinometylen)-4H-1,2,4-triazole-5-thioles. According to the results of computer prediction it was found that it is advisable to perform in vivo studies for these substances on the ability to use in the treatment of hastrinomy, ulcers, tuberculosis, atherosclerosis and for eradication of Helicobacter Pylori.В работе приведены результаты исследования антиоксидантной активности солей 2-((4-R-3-(морфолинометилен)-4H-1,2,4-триазол-5-ил)тио)уксусных кислот. Установлено, что калиевая соль 2-((3-(морфолинометилен)-4-амино-4H-1,2,4-триазол-5-ил)тио)уксусной кислоты (ПКР-173) по силе фармакологического действия превышает эталоны сравнения аскорбиновую кислоту и тиотриазолин. Отмечено перспективность дальнейшей химической модификации солей 2-((4-R-3-(морфолинометилен)-4H-1,2,4-триазол-5-ил)тио)уксусных кислот и установлены некоторые закономерности зависимости «структура - действие».В роботі наведені результати дослідження антиоксидантної активності солей 2-((4-R-3-(морфолінометилен)-4H-1,2,4-тріазол-5-іл)тіо)ацетатних кислот. Встановлено, що калієва сіль 2-((3-(морфолінометилен)-4-аміно-4H-1,2,4-тріазол-5-іл)тіо)ацетатної кислоти (ПКР-173) за силою фармакологічної дії перевищує еталони порівняння аскорбінову кислоту та тіотріазолін. Відмічено перспективність подальшої хімічної модифікації солей 2-((4-R-3-(морфолінометилен)-4H-1,2,4-тріазол-5-іл)тіо)ацетатних кислот та встановлені деякі закономірності залежності «структура - дія»

Дослідження впливу солей 2-((4-R-3-(морфолінометилен)-4H-1,2,4-триазол-5-іл) тіо)ацетатних кислот на ріст і розвиток паростків кукурудзи

Topicality. Agricultural industry urgently requires new and effective growth stimulating remedies. 1,2,4-triazole derivatives have had exhibited themselves as active fungicides and growth stimulators and the salts of 2-(4-R-3-R1-1,2,4-triazole-5-yltio)acetic acid are quite promising in this aspect.Aim. To determine the impact on quality indicators of Galatea hybrid corn sprouts germination after the processing with solutions of 2-((4-R-3 (morfolinomethylen)-4H-1,2,4-triazole-5-yl)thio) acetic acid salts.Materials and methods. The objects of our research were 10 new substances derivative 1,2,4-triazole derivatives. Further it was studied the impact of these compounds on the performance and germination of the “Galatea” hybrid corn seed in 2016 harvest. We have used auxin as the study comparison and distilled water was used as a control.Results and discussion. The study had found that these compounds could differently influence on the growth and development of corn sprouts. It was mentioned that on the growth stimulating activity intensiveness can influence the replacement of amino group at the N4 nitrogen atom of 1,2,4-triazole cycle and the type of cation which is combined with acids.Conclusions. In the result of our experiment it was determined the prospects of further investigations of synthesized compounds as a growth stimulators and noted appropriateness of “structure action” dependences could be integrated into future research.Актуальность. Сельскохозяйственная промышленность остро нуждается в создании новых и эффективных ростстимулирующих средств. Производные 1,2,4-триазола уже успели проявить себя как активные стимуляторы роста и фунгициды, а соли 2-(4-R-3-R1-1,2,4-триазол-5-илтио)ацетатных кислот являются весьма перспективными в этом плане.Целью данных исследований является определение влияния на качественные показатели прорастания ростков кукурузы гибрида Галатея после их обработки растворами солей 2-((4-R-3-(морфолинометилен)-4H-1,2,4-триазол-5-ил)тио)ацетатных кислот.Материалы и методы. Объектами наших исследований были 10 новых веществ, производных 1,2,4-триазола. В дальнейшем проведено исследование влияния указанных соединений на показатели энергии прорас-тания и всхожести семян кукурузы гибрида «Галатея» урожая 2016 г. Как эталон исследования использовался ауксин, а контролем служила дистиллированная вода.Результаты и их обсуждение. В результате исследования установлено, что указанные соединения поразному способны влиять на рост и развитие ростков кукурузы. Отмечено, что на интенсивность ростстимулирующей активности влияют как заместители при N4 атоме азота 1,2,3,4-триазолового цикла, так и характер катиона, который связан с кислотами.Выводы. В результате эксперимента установлено перспективность дальнейших исследований синтезированных веществ в качестве ростстимуляторов, а отмеченные закономерности зависимости «структура-действие» могут быть интегрированы в дальнейшие исследования.Актуальність. Сільськогосподарська промисловість гостро потребує створення нових та ефективних ріст-стимулюючих засобів. Похідні 1,2,4-триазолу вже встигли проявити себе як активні стимулятори росту та фунгіциди, а солі 2-(4-R-3-R1-1,2,4-триазол-5-ілтіо)ацетатних кислот є досить перспективними в цьому плані.Метою даних досліджень є визначення впливу на якісні показники проростання паростків кукурудзи гібриду Галатея після їх обробки розчинами солей 2-((4-R-3-(морфолінометилен)-4H-1,2,4-триазол-5-іл)тіо)ацетатних кислот.Матеріали та методи. Об’єктами наших досліджень були 10 нових речовин, похідних 1,2,4-триазолу. В подальшому проведено дослідження впливу вказаних сполук на показники енергії проростання та схожості насіння кукурудзи гібриду «Галатея» врожаю 2016 р. Як еталон дослідження використовувався ауксин, а контролем слугувала дистильована вода.Результати та їх обговорення. В результаті проведеного дослідження встановлено, що вказані сполуки по-різному здатні впливати на ріст та розвиток паростків кукурудзи. Відмічено, що на інтенсивність рістстиму-люючої активності впливають як замісники за N4 атомом азоту 1,2,4-триазолового циклу, так і характер катіону зв’язаного з кислотами.Висновки. В результаті експерименту встановлено перспективність подальших досліджень синтезованих речовин в якості рістстимуляторів, а відмічені закономірності залежності «структура-дія» можуть бути інтегровані в подальші дослідження

Measurements of the branching fractions for B→K∗γB \to K^{*}\gamma decays at Belle II

This paper reports a study of $B \to K^{*}\gamma$ decays using $62.8\pm 0.6$ fb$^{-1}$ of data collected during 2019--2020 by the Belle II experiment at the SuperKEKB $e^{+}e^{-}$ asymmetric-energy collider, corresponding to $(68.2 \pm 0.8) \times 10^6$ $B\overline{B}$ events. We find $454 \pm 28$, $50 \pm 10$, $169 \pm 18$, and $160 \pm 17$ signal events in the decay modes $B^{0} \to K^{*0}[K^{+}\pi^{-}]\gamma$, $B^{0} \to K^{*0}[K^0_{\rm S}\pi^{0}]\gamma$, $B^{+} \to K^{*+}[K^{+}\pi^{0}]\gamma$, and $B^{+} \to K^{*+}[K^{+}\pi^{0}]\gamma$, respectively. The uncertainties quoted for the signal yield are statistical only. We report the branching fractions of these decays: $$\mathcal{B} [B^{0} \to K^{*0}[K^{+}\pi^{-}]\gamma] = (4.5 \pm 0.3 \pm 0.2) \times 10^{-5},$$ $$\mathcal{B} [B^{0} \to K^{*0}[K^0_{\rm S}\pi^{0}]\gamma] = (4.4 \pm 0.9 \pm 0.6) \times 10^{-5},$$ $$\mathcal{B} [B^{+} \to K^{*+}[K^{+}\pi^{0}]\gamma] = (5.0 \pm 0.5 \pm 0.4)\times 10^{-5},\text{ and}$$ $$\mathcal{B} [B^{+} \to K^{*+}[K^0_{\rm S}\pi^{+}]\gamma] = (5.4 \pm 0.6 \pm 0.4) \times 10^{-5},$$ where the first uncertainty is statistical, and the second is systematic. The results are consistent with world-average values

Measurement of the integrated luminosity of the Phase 2 data of the Belle II experiment

From April to July 2018, a data sample at the peak energy of the γ(4S) resonance was collected with the Belle II detector at the SuperKEKB electron-positron collider. This is the first data sample of the Belle II experiment. Using Bhabha and digamma events, we measure the integrated luminosity of the data sample to be (496.3 ± 0.3 ± 3.0) pb-1, where the first uncertainty is statistical and the second is systematic. This work provides a basis for future luminosity measurements at Belle II

Angular analysis of B+→ρ+ρ0B^+ \to \rho^+\rho^0 decays reconstructed in 2019, 2020, and 2021 Belle II data

We report on a Belle II measurement of the branching fraction ($\mathcal{B}$), longitudinal polarization fraction ($f_L$), and CP asymmetry ($\mathcal{A}_{CP}$) of $B^+\to \rho^+\rho^0$ decays. We reconstruct $B^+\to \rho^+(\to \pi^+\pi^0(\to \gamma\gamma))\rho^0(\to \pi^+\pi^-)$ decays in a sample of SuperKEKB electron-positron collisions collected by the Belle II experiment in 2019, 2020, and 2021 at the $\Upsilon$(4S) resonance and corresponding to 190 fb$^{-1}$ of integrated luminosity. We fit the distributions of the difference between expected and observed $B$ candidate energy, continuum-suppression discriminant, dipion masses, and decay angles of the selected samples, to determine a signal yield of $345 \pm 31$ events. The signal yields are corrected for efficiencies determined from simulation and control data samples to obtain $\mathcal{B}(B^+ \to \rho^+\rho^0) = [23.2^{+\ 2.2}_{-\ 2.1} (\rm stat) \pm 2.7 (\rm syst)]\times 10^{-6}$,$f_L = 0.943 ^{+\ 0.035}_{-\ 0.033} (\rm stat)\pm 0.027(\rm syst)$, and$\mathcal{A}_{CP}=-0.069 \pm 0.068(\rm stat) \pm 0.060 (\rm syst)$. The results agree with previous measurements. This is the first measurement of$\mathcal{A}_{CP}$in$B^+\to \rho^+\rho^0$ decays reported by Belle II

Determination of ∣Vub∣|V_{ub}| from untagged B0→π−ℓ+νℓB^0\to\pi^- \ell^+ \nu_{\ell} decays using 2019-2021 Belle II data

We present an analysis of the charmless semileptonic decay $B^0\to\pi^- \ell^+ \nu_{\ell}$, where $\ell = e, \mu$, from 198.0 million pairs of $B\bar{B}$ mesons recorded by the Belle II detector at the SuperKEKB electron-positron collider. The decay is reconstructed without identifying the partner $B$ meson. The partial branching fractions are measured independently for $B^0\to\pi^- e^+ \nu_{e}$ and $B^0\to\pi^- \mu^+ \nu_{\mu}$ as functions of $q^{2}$ (momentum transfer squared), using 3896 $B^0\to\pi^- e^+ \nu_{e}$ and 5466 $B^0\to\pi^- \mu^+ \nu_{\mu}$ decays. The total branching fraction is found to be $(1.426 \pm 0.056 \pm 0.125) \times 10^{-4}$ for $B^0\to\pi^- \ell^+ \nu_{\ell}$ decays, where the uncertainties are statistical and systematic, respectively. By fitting the measured partial branching fractions as functions of $q^{2}$, together with constraints on the nonperturbative hadronic contribution from lattice QCD calculations, the magnitude of the Cabibbo-Kobayashi-Maskawa matrix element $V_{ub}$, $(3.55 \pm 0.12 \pm 0.13 \pm 0.17) \times 10^{-3}$, is extracted. Here, the first uncertainty is statistical, the second is systematic and the third is theoretical