60 research outputs found

    pH, Total Bacteria and Total Fungi Litter Fermentation at Different Ripening Durations

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    This study aims to examine the effect of fermentation time on pH levels, total bacteria and total fungi litter chicken fermented. The research method was carried out by collecting various chicken litters from 16 closed house cages in Semarang City, Demak Regency and Kendal Regency, then combined and fermented. The study used a completely randomized design in the direction of 4 treatments and 4 replications, the treatments were T0 = 0 week litter curing; T1 = 3 weeks litter curing; T2 = 6 weeks of litter curing; T3 = 9 weeks litter curing. The parameters observed were pH value, total bacteria and total litter fungi in broiler chickens. The results showed that there was a significant effect (P 0.05) on all treatments. The conclusion of this research is the best chicken litter fermentation at 6 weeks duration of ripening. Produce a total of bacteria and fungi as much as 0.25 x 103 CFU/g and indicated that they were not pathogenic bacteria and fungi

    Respon Pertumbuhan Dan Produksi Semangka (Citrullus Vulgaris Schard.) Terhadap Pemberian Pupuk NPK(15:15:15) Dan Pemangkasan Buah

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    Pemberian pupuk NPK dan pemangkasan buah berpengaruh terhadap pertumbuhan dan produksisemangka. Penelitian ini bertujuan untuk mendapatkan dosis pupuk NPK yang tepat danpemangkasan buah yang sesuai untuk pertumbuhan dan produksi semangka. Penelitian dilakukan dilahan masyarakat, Dusun Sei Mencirim Kecamatan Sunggal Kabupaten Deli Serdang, mulai bulanApril sampai Juli 2013, menggunakan Rancangan Acak Kelompok faktorial dengan 2 faktor. Faktorpertama adalah Dosis pupuk NPK (0, 40, 80, 120 gram) sedangkan faktor kedua adalah jumlah buahper tanaman (1, 2, 3 buah per tanaman). Parameter yang diamati adalah panjang tanaman, jumlahcabang primer dan sekunder, berat buah, panjang buah, diameter buah, produksi per tanaman,produksi per plot, produksi per hektar, dan mutu buah.Hasil penelitian diperoleh bahwa perlakuandosis pupuk NPK berpengaruh nyata terhadap parameter panjang sulur umur 6 – 8 MST, jumlahcabang primer dan sekunder umur 5 MST, panjang buah, diameter buah, berat buah, produksipertanaman, produksi per plot, produksi per hektar dan mutu buah kelas A, B dan C. Jumlah buahper tanaman berpengaruh nyata panjang buah, diameter buah, berat buah, produksi pertanaman,produksi per plot, produksi per hektar dan mutu buah kelas A, B dan C. Sedangkan interaksi antaradosis pupuk NPK dan jumlah buah per tanaman berpengaruh nyata terhadap produksi per tanaman,produksi per plot dan per hektar

    Boundary friction characterisation of a used cylinder liner subject to fired engine conditions and surface deposition

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    In cylinder friction contributes as a primary source of parasitic dissipations in IC engines. For future engines to become more efficient, with enhanced fuel economy and increased power output, accurate prediction of new designs is required over the full lifetime of an engine. The work carried out presents use of a local pressure coefficient of boundary shear strength of asperities value, taking into account the localised effects of surface texture, coating and surface deposition. XPS spectra analysis was also carried out to identify the surface depositions as a result of combustion, not previously taken into account during piston ring pack simulation. Friction was shown by simulation to drop by up to 30% between the compression and combustion stroke as a result of using a carriable coefficient of boundary shear strength of asperities. It was found that piston varnish on the liner corresponded to higher values of the pressure coefficient of boundary shear strength of asperities, therefore showing the importance of using real system components run under representative operating conditions or numerical analyses

    Redescription of Cosmocephalus tanakai

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    THE DIFFERENCES OF ANTITHROMBIN III, FIBRINOGEN, AND TROPONIN I LEVELS BETWEEN ACUTE ISCHEMIC STROKE AND ACUTE HEMORRHAGIC STROKE

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    Introduction: Plasma antithrombin III associated with fibrinogen might help the risk assessment of acute ischemic stroke, but studies that discuss those levels in hemorrhagic stroke are still limited. Troponin I is a cardiac enzyme that has high sensitivity and specificity in the detection of heart injury after stroke. The purpose of this study is to determine the differences of antithrombin III, fibrinogen, and troponin I levels between acute ischemic stroke and acute hemorrhagic stroke. Method: This study used a descriptive analytic study with a cross sectional design. A total of 52 research subjects, consisting of 26 acute ischemic stroke patients and 26 acute hemorrhagic stroke patients were taken by consecutive non-random sampling method. The blood samples from the subjects that have been diagnosed by history taking, physical examination and head CT scan, were taken for examination of antithrombin III, fibrinogen, and troponin I levels. Data analysis was performed by unpaired T test and Mann-Whitney test. Results: The median antithrombin III level in the acute ischemic stroke group was 93.00%, while in the acute hemorrhagic stroke group was 101.85% (p=0.341). The mean fibrinogen level in the acute ischemic stroke group was 453.46 Β± 171.16 mg/dL, while in the acute hemorrhagic stroke group was 399.15 Β± 203.02 mg/dL (p=0.302). The median troponin I level in the acute ischemic stroke group was 0.00 ng/mL, while in the acute hemorrhagic stroke group was 0.00 ng/mL (p=0.698). Conclusion: There were no significant differences of antithrombin III, fibrinogen, and troponin I levels between acute ischemic stroke and acute hemorrhagic stroke

    CΠΈΠ½Ρ‚Π΅Π· Ρ‚Π° Π³Ρ–ΠΏΠΎΠ³Π»Ρ–ΠΊΠ΅ΠΌΡ–Ρ‡Π½Π° Π°ΠΊΡ‚ΠΈΠ²Π½Ρ–ΡΡ‚ΡŒ ΠΏΠΎΡ…Ρ–Π΄Π½ΠΈΡ… 4-ΠΏΡ–Ρ€Π°Π·ΠΎΠ»Ρ–Π΄Π΅Π½-3-ΠΊΠ°Ρ€Π±ΠΎΠ½ΠΎΠ²ΠΈΡ… кислот, Π΅ΠΊΠ·ΠΎΡ„ΡƒΠ½ΠΊΡ†Ρ–ΠΎΠ½Π°Π»Ρ–Π·ΠΎΠ²Π°Π½ΠΈΡ… Π³Ρ–Π΄Ρ€Π°Π·ΠΈΠ½Ρ–Π»Ρ–Π΄Π΅Π½-1,3-Ρ‚Ρ–Π°Π·ΠΎΠ»Ρ–Π΄ΠΈΠ½ΠΎΠ²ΠΈΠΌ Ρ„Ρ€Π°Π³ΠΌΠ΅Π½Ρ‚ΠΎΠΌ

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    It has been shown that 4- formylpyrazole-3-carboxylic acids and their ethyl esters interact selectively with thiosemicarbazide and its N4-aryl-derivatives in boiling acetic acid with formation of the corresponding 4-pyrazolylthiosemicarbazones with the yields of 76-91%. It has been found that heating of 4-pyrazolylthiosemicarbazones with diethyl acetylenedicarboxylate in boiling ethanol for 3 hours leads to formation of 1,3-thiazolidine-containing polyfunctional pyrazole derivatives with yields of 73-95%. Formation of compounds of this type indicates that the process occurs according to the scheme of the primary attack of a highly electrophilic triple bond of acetylenedicarboxylate by the nucleophilic atom of sulfur of the thiosemicarbazone fragment with subsequent intramolecular condensation, which leads to formation of the 4-oxo-1,3-thiazolidine-5-ilidene cycle. The structure of the 1,3-thiazolidinilidenehydrazonepyrazoles synthesized has been proven by a complex of spectral methods; the most informative of them are 13CΒ NMR spectra with signals of carbon atoms of the thiazolidine cycle: C4 (159-161 ppm), C2 (162-165 ppm), C5 (163-165 ppm), as well as of the exo-cyclic ethoxycarbonylethylidene fragment: HC= (114-118 ppm); and of C(O) O (165 ppm). It has been determined that the compounds synthesized cause the hypoglycemic dose-dependent effect in mice, which is much more potent than the same effect of the reference medicine – pioglitazone.Показано, Ρ‡Ρ‚ΠΎ 4-Ρ„ΠΎΡ€ΠΌΠΈΠ»ΠΏΠΈΡ€Π°Π·ΠΎΠ»-3-ΠΊΠ°Ρ€Π±ΠΎΠ½ΠΎΠ²Ρ‹Π΅ кислоты ΠΈ ΠΈΡ… этиловыС эфиры сСлСктивно Π²Π·Π°ΠΈΠΌΠΎΠ΄Π΅ΠΉΡΡ‚Π²ΡƒΡŽΡ‚ с тиосСмикарбазидом ΠΈ Π΅Π³ΠΎ N4-Π°Ρ€ΠΈΠ»ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹ΠΌΠΈ Π² кипящСй уксусной кислотС с ΠΎΠ±Ρ€Π°Π·ΠΎΠ²Π°Π½ΠΈΠ΅ΠΌ ΠΈ Π²Ρ‹Ρ…ΠΎΠ΄Π°ΠΌΠΈ 76-91% ΡΠΎΠΎΡ‚Π²Π΅Ρ‚ΡΡ‚Π²ΡƒΡŽΡ‰ΠΈΡ… 4-пиразолилтиосСмкарбазонов. НайдСно, Ρ‡Ρ‚ΠΎ 3-часовоС Π½Π°Π³Ρ€Π΅Π²Π°Π½ΠΈΠ΅ послСдних с диэтилацСтилСндикарбоксилатом Π² кипящСм этанолС ΠΏΡ€ΠΈΠ²ΠΎΠ΄ΠΈΡ‚ ΠΊ 1,3-тиазолидинсодСрТащим ΠΏΠΎΠ»ΠΈΡ„ΡƒΠ½ΠΊΡ†ΠΈΠΎΠ½Π°Π»ΡŒΠ½Ρ‹ΠΌ ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹ΠΌ ΠΏΠΈΡ€Π°Π·ΠΎΠ»Π° с Π²Ρ‹Ρ…ΠΎΠ΄Π°ΠΌΠΈ 73-95%. ΠžΠ±Ρ€Π°Π·ΠΎΠ²Π°Π½ΠΈΠ΅ Ρ‚Π°ΠΊΠΎΠ³ΠΎ Ρ‚ΠΈΠΏΠ° соСдинСний ΡΠ²ΠΈΠ΄Π΅Ρ‚Π΅Π»ΡŒΡΡ‚Π²ΡƒΠ΅Ρ‚ ΠΎ Ρ‚ΠΎΠΌ, Ρ‡Ρ‚ΠΎ процСсс рСализуСтся ΠΏΠΎ схСмС ΠΏΠ΅Ρ€Π²ΠΈΡ‡Π½ΠΎΠΉ Π°Ρ‚Π°ΠΊΠΈ Π½ΡƒΠΊΠ»Π΅ΠΎΡ„ΠΈΠ»ΡŒΠ½ΠΎΠ³ΠΎ Π°Ρ‚ΠΎΠΌΠ° сСры тиосСмикарбазонного Ρ„Ρ€Π°Π³ΠΌΠ΅Π½Ρ‚Π° Π½Π° Π²Ρ‹ΡΠΎΠΊΠΎΡΠ»Π΅ΠΊΡ‚Ρ€ΠΎΡ„ΠΈΠ»ΡŒΠ½ΡƒΡŽ Ρ‚Ρ€ΠΎΠΉΠ½ΡƒΡŽ связь ацСтилСндикарбоксилата с ΠΏΠΎΡΠ»Π΅Π΄ΡƒΡŽΡ‰Π΅ΠΉ внутримолСкулярной кондСнсациСй, которая ΠΏΡ€ΠΈΠ²ΠΎΠ΄ΠΈΡ‚ ΠΊ Ρ„ΠΎΡ€ΠΌΠΈΡ€ΠΎΠ²Π°Π½ΠΈΡŽ 4-оксо-1,3-Ρ‚ΠΈΠ°Π·ΠΎΠ»ΠΈΠ΄ΠΈΠ½-5-ΠΈΠ»ΠΈΠ΄Π΅Π½ΠΎΠ²ΠΎΠ³ΠΎ Ρ†ΠΈΠΊΠ»Π°. Π‘Ρ‚Ρ€ΡƒΠΊΡ‚ΡƒΡ€Π° ΠΏΠΎΠ»ΡƒΡ‡Π΅Π½Π½Ρ‹Ρ… 1,3-Ρ‚ΠΈΠ°Π·ΠΎΠ»ΠΈΠ΄ΠΈΠ½ΠΈΠ»ΠΈΠ΄Π΅Π½Π³ΠΈΠ΄Ρ€Π°Π·ΠΎΠ½ΠΎΠΏΠΈΡ€Π°Π·ΠΎΠ»ΠΎΠ² установлСна комплСксом ΡΠΏΠ΅ΠΊΡ‚Ρ€Π°Π»ΡŒΠ½Ρ‹Ρ… ΠΌΠ΅Ρ‚ΠΎΠ΄ΠΎΠ², Π½Π°ΠΈΠ±ΠΎΠ»Π΅Π΅ ΠΈΠ½Ρ„ΠΎΡ€ΠΌΠ°Ρ‚ΠΈΠ²Π½Ρ‹ΠΌΠΈ ΠΈΠ· ΠΊΠΎΡ‚ΠΎΡ€Ρ‹Ρ… ΡΠ²Π»ΡΡŽΡ‚ΡΡ спСктры ЯМР 13Π‘ с сигналами Π°Ρ‚ΠΎΠΌΠΎΠ² ΡƒΠ³Π»Π΅Ρ€ΠΎΠ΄Π° Ρ‚ΠΈΠ°Π·ΠΎΠ»ΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ Ρ†ΠΈΠΊΠ»Π°: C4 (159-161 ΠΌ.Ρ‡.), Π‘2 (162-165 ΠΌ.Ρ‡.), Π‘5 (163-165 ΠΌ.Ρ‡.), Π° Ρ‚Π°ΠΊΠΆΠ΅ экзоцикличСского этоксикарбонилэтилидСнового Ρ„Ρ€Π°Π³ΠΌΠ΅Π½Ρ‚Π°: НБ= (114-118 ΠΌ.Ρ‡.) ΠΈ Π‘(О)О (165 ΠΌ.Ρ‡.). УстановлСно, Ρ‡Ρ‚ΠΎ синтСзированныС соСдинСния Π²Ρ‹Π·Ρ‹Π²Π°ΡŽΡ‚ гипогликСмичСский дозозависимый эффСкт Ρƒ ΠΌΡ‹ΡˆΠ΅ΠΉ, ΠΊΠΎΡ‚ΠΎΡ€Ρ‹ΠΉ сущСствСнно ΠΏΡ€Π΅Π²Ρ‹ΡˆΠ°Π΅Ρ‚ ΡΠ°Ρ…Π°Ρ€ΠΎΡΠ½ΠΈΠΆΠ°ΡŽΡ‰Π΅Π΅ дСйствиС Ρ€Π΅Ρ„Π΅Ρ€Π΅Π½Ρ‚Π½ΠΎΠ³ΠΎ ΠΏΡ€Π΅ΠΏΠ°Ρ€Π°Ρ‚Π° ΠΏΠΈΠΎΠ³Π»ΠΈΡ‚Π°Π·ΠΎΠ½Π°.Показано, Ρ‰ΠΎ 4-Ρ„ΠΎΡ€ΠΌΡ–Π»ΠΏΡ–Ρ€Π°Π·ΠΎΠ»-3-ΠΊΠ°Ρ€Π±ΠΎΠ½ΠΎΠ²Ρ– кислоти Ρ‚Π° Ρ—Ρ… Π΅Ρ‚ΠΈΠ»ΠΎΠ²Ρ– СстСри сСлСктивно Π²Π·Π°Ρ”ΠΌΠΎΠ΄Ρ–ΡŽΡ‚ΡŒ Ρ–Π· тіосСмікарбазидом Ρ– ΠΉΠΎΠ³ΠΎ N4-Π°Ρ€ΠΈΠ»ΠΏΠΎΡ…Ρ–Π΄Π½ΠΈΠΌΠΈ Π² киплячій ΠΎΡ†Ρ‚ΠΎΠ²Ρ–ΠΉ кислоті Π· утворСнням Ρ– Π²ΠΈΡ…ΠΎΠ΄Π°ΠΌΠΈ 76-91% Π²Ρ–Π΄ΠΏΠΎΠ²Ρ–Π΄Π½ΠΈΡ… 4-ΠΏΡ–Ρ€Π°Π·ΠΎΠ»Ρ–Π»-тіосСмікарбазонів. Π—Π½Π°ΠΉΠ΄Π΅Π½ΠΎ, Ρ‰ΠΎ 3-Π³ΠΎΠ΄ΠΈΠ½Π½Π΅ нагрівання останніх Ρ–Π· діСтилацСтилСндикарбоксилатом Ρƒ киплячому Π΅Ρ‚Π°Π½ΠΎΠ»Ρ– ΠΏΡ€ΠΈΠ²ΠΎΠ΄ΠΈΡ‚ΡŒ Π΄ΠΎ 1,3-тіазолідиновмісних ΠΏΠΎΠ»Ρ–Ρ„ΡƒΠ½ΠΊΡ†Ρ–ΠΎΠ½Π°Π»ΡŒΠ½ΠΈΡ… ΠΏΠΎΡ…Ρ–Π΄Π½ΠΈΡ… ΠΏΡ–Ρ€Π°Π·ΠΎΠ»Ρƒ Π· Π²ΠΈΡ…ΠΎΠ΄Π°ΠΌΠΈ 73-95%. УтворСння Ρ‚Π°ΠΊΠΎΠ³ΠΎ Ρ‚ΠΈΠΏΡƒ сполук Ρ” свідчСнням Ρ‚ΠΎΠ³ΠΎ, Ρ‰ΠΎ процСс Ρ€Π΅Π°Π»Ρ–Π·ΡƒΡ”Ρ‚ΡŒΡΡ Π·Π° ΡΡ…Π΅ΠΌΠΎΡŽ ΠΏΠ΅Ρ€Π²ΠΈΠ½Π½ΠΎΡ— Π°Ρ‚Π°ΠΊΠΈ Π½ΡƒΠΊΠ»Π΅ΠΎΡ„Ρ–Π»ΡŒΠ½ΠΎΠ³ΠΎ Π°Ρ‚ΠΎΠΌΠ° сірки тіосСмікарбазонного Ρ„Ρ€Π°Π³ΠΌΠ΅Π½Ρ‚Π° Π½Π° Π²ΠΈΡΠΎΠΊΠΎΠ΅Π»Π΅ΠΊΡ‚Ρ€ΠΎΡ„Ρ–Π»ΡŒΠ½ΠΈΠΉ ΠΏΠΎΡ‚Ρ€Ρ–ΠΉΠ½ΠΈΠΉ зв’язок ацСтилСндикарбоксилату Ρ–Π· подальшою Π²Π½ΡƒΡ‚Ρ€Ρ–ΡˆΠ½ΡŒΠΎΠΌΠΎΠ»Π΅ΠΊΡƒΠ»ΡΡ€Π½ΠΎΡŽ ΠΊΠΎΠ½Π΄Π΅Π½ΡΠ°Ρ†Ρ–Ρ”ΡŽ, яка ΠΏΡ€ΠΈΠ²ΠΎΠ΄ΠΈΡ‚ΡŒ Π΄ΠΎ формування 4-оксо-1,3-Ρ‚Ρ–Π°Π·ΠΎΠ»Ρ–Π΄ΠΈΠ½-5-Ρ–Π»Ρ–Π΄Π΅Π½ΠΎΠ²ΠΎΠ³ΠΎ Ρ†ΠΈΠΊΠ»Ρƒ. Π‘Ρ‚Ρ€ΡƒΠΊΡ‚ΡƒΡ€Π° ΠΎΡ‚Ρ€ΠΈΠΌΠ°Π½ΠΈΡ… 1,3-Ρ‚Ρ–Π°Π·ΠΎΠ»Ρ–Π΄ΠΈΠ½Ρ–Π»Ρ–Π΄Π΅Π½Π³Ρ–Π΄Ρ€Π°Π·ΠΎΠ½ΠΎΠΏΡ–Ρ€Π°Π·ΠΎΠ»Ρ–Π² Π΄ΠΎΠ²Π΅Π΄Π΅Π½Π° комплСксом ΡΠΏΠ΅ΠΊΡ‚Ρ€Π°Π»ΡŒΠ½ΠΈΡ… ΠΌΠ΅Ρ‚ΠΎΠ΄Ρ–Π², Π½Π°ΠΉΡ–Π½Ρ„ΠΎΡ€ΠΌΠ°Ρ‚ΠΈΠ²Π½Ρ–ΡˆΠΈΠΌΠΈ Π· яких Ρ” спСктри ЯМР 13Π‘ Ρ–Π· сигналами Π°Ρ‚ΠΎΠΌΡ–Π² Π²ΡƒΠ³Π»Π΅Ρ†ΡŽ Ρ‚Ρ–Π°Π·ΠΎΠ»Ρ–Π΄ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ Ρ†ΠΈΠΊΠ»Ρƒ: C4 (159-161 ΠΌ.Ρ‡.), Π‘2 (162-165 ΠΌ.Ρ‡.), Π‘5 (163-165 ΠΌ.Ρ‡.), Π° Ρ‚Π°ΠΊΠΎΠΆ Π΅ΠΊΠ·ΠΎΡ†ΠΈΠΊΠ»Ρ–Ρ‡Π½ΠΎΠ³ΠΎ СтоксикарбонілСтилідСнового Ρ„Ρ€Π°Π³ΠΌΠ΅Π½Ρ‚Π°: НБ= (114-118 ΠΌ.Ρ‡.) Ρ‚Π° Π‘(О)О (165 ΠΌ.Ρ‡.). ВстановлСно, Ρ‰ΠΎ синтСзовані сполуки Π²ΠΈΠΊΠ»ΠΈΠΊΠ°ΡŽΡ‚ΡŒ Π³Ρ–ΠΏΠΎΠ³Π»Ρ–ΠΊΠ΅ΠΌΡ–Ρ‡Π½ΠΈΠΉ Π΄ΠΎΠ·ΠΎΠ·Π°Π»Π΅ΠΆΠ½ΠΈΠΉ Π΅Ρ„Π΅ΠΊΡ‚ Ρƒ мишСй, який суттєво ΠΏΠ΅Ρ€Π΅Π²ΠΈΡ‰ΡƒΡ” Ρ†ΡƒΠΊΡ€ΠΎΠ·Π½ΠΈΠΆΡƒΠ²Π°Π»ΡŒΠ½Ρƒ Π΄Ρ–ΡŽ Ρ€Π΅Ρ„Π΅Ρ€Π΅Π½Ρ‚Π½ΠΎΠ³ΠΎ ΠΏΡ€Π΅ΠΏΠ°Ρ€Π°Ρ‚Ρƒ ΠΏΡ–ΠΎΠ³Π»Ρ–Ρ‚Π°Π·ΠΎΠ½Ρƒ

    CΠΈΠ½Ρ‚Π΅Π· Ρ‚Π° Π³Ρ–ΠΏΠΎΠ³Π»Ρ–ΠΊΠ΅ΠΌΡ–Ρ‡Π½Π° Π°ΠΊΡ‚ΠΈΠ²Π½Ρ–ΡΡ‚ΡŒ ΠΏΠΎΡ…Ρ–Π΄Π½ΠΈΡ… 4-ΠΏΡ–Ρ€Π°Π·ΠΎΠ»Ρ–Π΄Π΅Π½-3-ΠΊΠ°Ρ€Π±ΠΎΠ½ΠΎΠ²ΠΈΡ… кислот, Π΅ΠΊΠ·ΠΎΡ„ΡƒΠ½ΠΊΡ†Ρ–ΠΎΠ½Π°Π»Ρ–Π·ΠΎΠ²Π°Π½ΠΈΡ… Π³Ρ–Π΄Ρ€Π°Π·ΠΈΠ½Ρ–Π»Ρ–Π΄Π΅Π½-1,3-Ρ‚Ρ–Π°Π·ΠΎΠ»Ρ–Π΄ΠΈΠ½ΠΎΠ²ΠΈΠΌ Ρ„Ρ€Π°Π³ΠΌΠ΅Π½Ρ‚ΠΎΠΌ

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    It has been shown that 4- formylpyrazole-3-carboxylic acids and their ethyl esters interact selectively with thiosemicarbazide and its N4-aryl-derivatives in boiling acetic acid with formation of the corresponding 4-pyrazolylthiosemicarbazones with the yields of 76-91%. It has been found that heating of 4-pyrazolylthiosemicarbazones with diethyl acetylenedicarboxylate in boiling ethanol for 3 hours leads to formation of 1,3-thiazolidine-containing polyfunctional pyrazole derivatives with yields of 73-95%. Formation of compounds of this type indicates that the process occurs according to the scheme of the primary attack of a highly electrophilic triple bond of acetylenedicarboxylate by the nucleophilic atom of sulfur of the thiosemicarbazone fragment with subsequent intramolecular condensation, which leads to formation of the 4-oxo-1,3-thiazolidine-5-ilidene cycle. The structure of the 1,3-thiazolidinilidenehydrazonepyrazoles synthesized has been proven by a complex of spectral methods; the most informative of them are 13CΒ NMR spectra with signals of carbon atoms of the thiazolidine cycle: C4 (159-161 ppm), C2 (162-165 ppm), C5 (163-165 ppm), as well as of the exo-cyclic ethoxycarbonylethylidene fragment: HC= (114-118 ppm); and of C(O) O (165 ppm). It has been determined that the compounds synthesized cause the hypoglycemic dose-dependent effect in mice, which is much more potent than the same effect of the reference medicine – pioglitazone.Показано, Ρ‡Ρ‚ΠΎ 4-Ρ„ΠΎΡ€ΠΌΠΈΠ»ΠΏΠΈΡ€Π°Π·ΠΎΠ»-3-ΠΊΠ°Ρ€Π±ΠΎΠ½ΠΎΠ²Ρ‹Π΅ кислоты ΠΈ ΠΈΡ… этиловыС эфиры сСлСктивно Π²Π·Π°ΠΈΠΌΠΎΠ΄Π΅ΠΉΡΡ‚Π²ΡƒΡŽΡ‚ с тиосСмикарбазидом ΠΈ Π΅Π³ΠΎ N4-Π°Ρ€ΠΈΠ»ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹ΠΌΠΈ Π² кипящСй уксусной кислотС с ΠΎΠ±Ρ€Π°Π·ΠΎΠ²Π°Π½ΠΈΠ΅ΠΌ ΠΈ Π²Ρ‹Ρ…ΠΎΠ΄Π°ΠΌΠΈ 76-91% ΡΠΎΠΎΡ‚Π²Π΅Ρ‚ΡΡ‚Π²ΡƒΡŽΡ‰ΠΈΡ… 4-пиразолилтиосСмкарбазонов. НайдСно, Ρ‡Ρ‚ΠΎ 3-часовоС Π½Π°Π³Ρ€Π΅Π²Π°Π½ΠΈΠ΅ послСдних с диэтилацСтилСндикарбоксилатом Π² кипящСм этанолС ΠΏΡ€ΠΈΠ²ΠΎΠ΄ΠΈΡ‚ ΠΊ 1,3-тиазолидинсодСрТащим ΠΏΠΎΠ»ΠΈΡ„ΡƒΠ½ΠΊΡ†ΠΈΠΎΠ½Π°Π»ΡŒΠ½Ρ‹ΠΌ ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹ΠΌ ΠΏΠΈΡ€Π°Π·ΠΎΠ»Π° с Π²Ρ‹Ρ…ΠΎΠ΄Π°ΠΌΠΈ 73-95%. ΠžΠ±Ρ€Π°Π·ΠΎΠ²Π°Π½ΠΈΠ΅ Ρ‚Π°ΠΊΠΎΠ³ΠΎ Ρ‚ΠΈΠΏΠ° соСдинСний ΡΠ²ΠΈΠ΄Π΅Ρ‚Π΅Π»ΡŒΡΡ‚Π²ΡƒΠ΅Ρ‚ ΠΎ Ρ‚ΠΎΠΌ, Ρ‡Ρ‚ΠΎ процСсс рСализуСтся ΠΏΠΎ схСмС ΠΏΠ΅Ρ€Π²ΠΈΡ‡Π½ΠΎΠΉ Π°Ρ‚Π°ΠΊΠΈ Π½ΡƒΠΊΠ»Π΅ΠΎΡ„ΠΈΠ»ΡŒΠ½ΠΎΠ³ΠΎ Π°Ρ‚ΠΎΠΌΠ° сСры тиосСмикарбазонного Ρ„Ρ€Π°Π³ΠΌΠ΅Π½Ρ‚Π° Π½Π° Π²Ρ‹ΡΠΎΠΊΠΎΡΠ»Π΅ΠΊΡ‚Ρ€ΠΎΡ„ΠΈΠ»ΡŒΠ½ΡƒΡŽ Ρ‚Ρ€ΠΎΠΉΠ½ΡƒΡŽ связь ацСтилСндикарбоксилата с ΠΏΠΎΡΠ»Π΅Π΄ΡƒΡŽΡ‰Π΅ΠΉ внутримолСкулярной кондСнсациСй, которая ΠΏΡ€ΠΈΠ²ΠΎΠ΄ΠΈΡ‚ ΠΊ Ρ„ΠΎΡ€ΠΌΠΈΡ€ΠΎΠ²Π°Π½ΠΈΡŽ 4-оксо-1,3-Ρ‚ΠΈΠ°Π·ΠΎΠ»ΠΈΠ΄ΠΈΠ½-5-ΠΈΠ»ΠΈΠ΄Π΅Π½ΠΎΠ²ΠΎΠ³ΠΎ Ρ†ΠΈΠΊΠ»Π°. Π‘Ρ‚Ρ€ΡƒΠΊΡ‚ΡƒΡ€Π° ΠΏΠΎΠ»ΡƒΡ‡Π΅Π½Π½Ρ‹Ρ… 1,3-Ρ‚ΠΈΠ°Π·ΠΎΠ»ΠΈΠ΄ΠΈΠ½ΠΈΠ»ΠΈΠ΄Π΅Π½Π³ΠΈΠ΄Ρ€Π°Π·ΠΎΠ½ΠΎΠΏΠΈΡ€Π°Π·ΠΎΠ»ΠΎΠ² установлСна комплСксом ΡΠΏΠ΅ΠΊΡ‚Ρ€Π°Π»ΡŒΠ½Ρ‹Ρ… ΠΌΠ΅Ρ‚ΠΎΠ΄ΠΎΠ², Π½Π°ΠΈΠ±ΠΎΠ»Π΅Π΅ ΠΈΠ½Ρ„ΠΎΡ€ΠΌΠ°Ρ‚ΠΈΠ²Π½Ρ‹ΠΌΠΈ ΠΈΠ· ΠΊΠΎΡ‚ΠΎΡ€Ρ‹Ρ… ΡΠ²Π»ΡΡŽΡ‚ΡΡ спСктры ЯМР 13Π‘ с сигналами Π°Ρ‚ΠΎΠΌΠΎΠ² ΡƒΠ³Π»Π΅Ρ€ΠΎΠ΄Π° Ρ‚ΠΈΠ°Π·ΠΎΠ»ΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ Ρ†ΠΈΠΊΠ»Π°: C4 (159-161 ΠΌ.Ρ‡.), Π‘2 (162-165 ΠΌ.Ρ‡.), Π‘5 (163-165 ΠΌ.Ρ‡.), Π° Ρ‚Π°ΠΊΠΆΠ΅ экзоцикличСского этоксикарбонилэтилидСнового Ρ„Ρ€Π°Π³ΠΌΠ΅Π½Ρ‚Π°: НБ= (114-118 ΠΌ.Ρ‡.) ΠΈ Π‘(О)О (165 ΠΌ.Ρ‡.). УстановлСно, Ρ‡Ρ‚ΠΎ синтСзированныС соСдинСния Π²Ρ‹Π·Ρ‹Π²Π°ΡŽΡ‚ гипогликСмичСский дозозависимый эффСкт Ρƒ ΠΌΡ‹ΡˆΠ΅ΠΉ, ΠΊΠΎΡ‚ΠΎΡ€Ρ‹ΠΉ сущСствСнно ΠΏΡ€Π΅Π²Ρ‹ΡˆΠ°Π΅Ρ‚ ΡΠ°Ρ…Π°Ρ€ΠΎΡΠ½ΠΈΠΆΠ°ΡŽΡ‰Π΅Π΅ дСйствиС Ρ€Π΅Ρ„Π΅Ρ€Π΅Π½Ρ‚Π½ΠΎΠ³ΠΎ ΠΏΡ€Π΅ΠΏΠ°Ρ€Π°Ρ‚Π° ΠΏΠΈΠΎΠ³Π»ΠΈΡ‚Π°Π·ΠΎΠ½Π°.Показано, Ρ‰ΠΎ 4-Ρ„ΠΎΡ€ΠΌΡ–Π»ΠΏΡ–Ρ€Π°Π·ΠΎΠ»-3-ΠΊΠ°Ρ€Π±ΠΎΠ½ΠΎΠ²Ρ– кислоти Ρ‚Π° Ρ—Ρ… Π΅Ρ‚ΠΈΠ»ΠΎΠ²Ρ– СстСри сСлСктивно Π²Π·Π°Ρ”ΠΌΠΎΠ΄Ρ–ΡŽΡ‚ΡŒ Ρ–Π· тіосСмікарбазидом Ρ– ΠΉΠΎΠ³ΠΎ N4-Π°Ρ€ΠΈΠ»ΠΏΠΎΡ…Ρ–Π΄Π½ΠΈΠΌΠΈ Π² киплячій ΠΎΡ†Ρ‚ΠΎΠ²Ρ–ΠΉ кислоті Π· утворСнням Ρ– Π²ΠΈΡ…ΠΎΠ΄Π°ΠΌΠΈ 76-91% Π²Ρ–Π΄ΠΏΠΎΠ²Ρ–Π΄Π½ΠΈΡ… 4-ΠΏΡ–Ρ€Π°Π·ΠΎΠ»Ρ–Π»-тіосСмікарбазонів. Π—Π½Π°ΠΉΠ΄Π΅Π½ΠΎ, Ρ‰ΠΎ 3-Π³ΠΎΠ΄ΠΈΠ½Π½Π΅ нагрівання останніх Ρ–Π· діСтилацСтилСндикарбоксилатом Ρƒ киплячому Π΅Ρ‚Π°Π½ΠΎΠ»Ρ– ΠΏΡ€ΠΈΠ²ΠΎΠ΄ΠΈΡ‚ΡŒ Π΄ΠΎ 1,3-тіазолідиновмісних ΠΏΠΎΠ»Ρ–Ρ„ΡƒΠ½ΠΊΡ†Ρ–ΠΎΠ½Π°Π»ΡŒΠ½ΠΈΡ… ΠΏΠΎΡ…Ρ–Π΄Π½ΠΈΡ… ΠΏΡ–Ρ€Π°Π·ΠΎΠ»Ρƒ Π· Π²ΠΈΡ…ΠΎΠ΄Π°ΠΌΠΈ 73-95%. УтворСння Ρ‚Π°ΠΊΠΎΠ³ΠΎ Ρ‚ΠΈΠΏΡƒ сполук Ρ” свідчСнням Ρ‚ΠΎΠ³ΠΎ, Ρ‰ΠΎ процСс Ρ€Π΅Π°Π»Ρ–Π·ΡƒΡ”Ρ‚ΡŒΡΡ Π·Π° ΡΡ…Π΅ΠΌΠΎΡŽ ΠΏΠ΅Ρ€Π²ΠΈΠ½Π½ΠΎΡ— Π°Ρ‚Π°ΠΊΠΈ Π½ΡƒΠΊΠ»Π΅ΠΎΡ„Ρ–Π»ΡŒΠ½ΠΎΠ³ΠΎ Π°Ρ‚ΠΎΠΌΠ° сірки тіосСмікарбазонного Ρ„Ρ€Π°Π³ΠΌΠ΅Π½Ρ‚Π° Π½Π° Π²ΠΈΡΠΎΠΊΠΎΠ΅Π»Π΅ΠΊΡ‚Ρ€ΠΎΡ„Ρ–Π»ΡŒΠ½ΠΈΠΉ ΠΏΠΎΡ‚Ρ€Ρ–ΠΉΠ½ΠΈΠΉ зв’язок ацСтилСндикарбоксилату Ρ–Π· подальшою Π²Π½ΡƒΡ‚Ρ€Ρ–ΡˆΠ½ΡŒΠΎΠΌΠΎΠ»Π΅ΠΊΡƒΠ»ΡΡ€Π½ΠΎΡŽ ΠΊΠΎΠ½Π΄Π΅Π½ΡΠ°Ρ†Ρ–Ρ”ΡŽ, яка ΠΏΡ€ΠΈΠ²ΠΎΠ΄ΠΈΡ‚ΡŒ Π΄ΠΎ формування 4-оксо-1,3-Ρ‚Ρ–Π°Π·ΠΎΠ»Ρ–Π΄ΠΈΠ½-5-Ρ–Π»Ρ–Π΄Π΅Π½ΠΎΠ²ΠΎΠ³ΠΎ Ρ†ΠΈΠΊΠ»Ρƒ. Π‘Ρ‚Ρ€ΡƒΠΊΡ‚ΡƒΡ€Π° ΠΎΡ‚Ρ€ΠΈΠΌΠ°Π½ΠΈΡ… 1,3-Ρ‚Ρ–Π°Π·ΠΎΠ»Ρ–Π΄ΠΈΠ½Ρ–Π»Ρ–Π΄Π΅Π½Π³Ρ–Π΄Ρ€Π°Π·ΠΎΠ½ΠΎΠΏΡ–Ρ€Π°Π·ΠΎΠ»Ρ–Π² Π΄ΠΎΠ²Π΅Π΄Π΅Π½Π° комплСксом ΡΠΏΠ΅ΠΊΡ‚Ρ€Π°Π»ΡŒΠ½ΠΈΡ… ΠΌΠ΅Ρ‚ΠΎΠ΄Ρ–Π², Π½Π°ΠΉΡ–Π½Ρ„ΠΎΡ€ΠΌΠ°Ρ‚ΠΈΠ²Π½Ρ–ΡˆΠΈΠΌΠΈ Π· яких Ρ” спСктри ЯМР 13Π‘ Ρ–Π· сигналами Π°Ρ‚ΠΎΠΌΡ–Π² Π²ΡƒΠ³Π»Π΅Ρ†ΡŽ Ρ‚Ρ–Π°Π·ΠΎΠ»Ρ–Π΄ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ Ρ†ΠΈΠΊΠ»Ρƒ: C4 (159-161 ΠΌ.Ρ‡.), Π‘2 (162-165 ΠΌ.Ρ‡.), Π‘5 (163-165 ΠΌ.Ρ‡.), Π° Ρ‚Π°ΠΊΠΎΠΆ Π΅ΠΊΠ·ΠΎΡ†ΠΈΠΊΠ»Ρ–Ρ‡Π½ΠΎΠ³ΠΎ СтоксикарбонілСтилідСнового Ρ„Ρ€Π°Π³ΠΌΠ΅Π½Ρ‚Π°: НБ= (114-118 ΠΌ.Ρ‡.) Ρ‚Π° Π‘(О)О (165 ΠΌ.Ρ‡.). ВстановлСно, Ρ‰ΠΎ синтСзовані сполуки Π²ΠΈΠΊΠ»ΠΈΠΊΠ°ΡŽΡ‚ΡŒ Π³Ρ–ΠΏΠΎΠ³Π»Ρ–ΠΊΠ΅ΠΌΡ–Ρ‡Π½ΠΈΠΉ Π΄ΠΎΠ·ΠΎΠ·Π°Π»Π΅ΠΆΠ½ΠΈΠΉ Π΅Ρ„Π΅ΠΊΡ‚ Ρƒ мишСй, який суттєво ΠΏΠ΅Ρ€Π΅Π²ΠΈΡ‰ΡƒΡ” Ρ†ΡƒΠΊΡ€ΠΎΠ·Π½ΠΈΠΆΡƒΠ²Π°Π»ΡŒΠ½Ρƒ Π΄Ρ–ΡŽ Ρ€Π΅Ρ„Π΅Ρ€Π΅Π½Ρ‚Π½ΠΎΠ³ΠΎ ΠΏΡ€Π΅ΠΏΠ°Ρ€Π°Ρ‚Ρƒ ΠΏΡ–ΠΎΠ³Π»Ρ–Ρ‚Π°Π·ΠΎΠ½Ρƒ

    Potential risks and pharmacological safety features of hypoglycemic drugs

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    For the treatment of diabetes, insulin preparations, synthetic hypoglycemic agents, herbal medicine and compulsory adherence to the diet. Oral hypoglycemic agents belong to different chemical classes: sulfonylurea derivatives, biguanides, thiazolidinediones, etc. They can also be divided into secretogens (stimulate pancreatic insulin secretion, especially in the presence of glucose) and prandial (food - related) glycemic regulators (lower glucose in the blood after eating). As for the pharmacological safety of oral antidiabetic agents, they are incompatible with adrenal cortex hormones, adrenomimetics, MAO inhibitors, psychostimulants, antiarrhythmic agents. Their hypoglycemic effect is weakened by estrogens, gestagens, oral contraceptives, chlorpromazine, barbiturates, phenothiazines, thyroid hormones, glucagon, lithium salts, saluretics, indomethacin, drugs containing nicotinic acid
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