А 72 Антиагрегационные свойства соединений класса 1, 3,4-тиадиазина= Platelet aggrega-tion inhibitor properties of 1,3,4-thiadiazine thiadiazines [] / Т. М. Васильева, В. А. Макаров, О. Н. Чупахин, Л. П. Сидорова, Н. М. Перова, В. Л. Русинов // Гематология и трансфузиология. - 2008. - Т. 53, № 4. - С. 12-14 : табл. - Библиогр.: с. 14 (14 назв.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: Исследовано влияние новых соединений, принадлежащих к классу 1,3,4-тиадиа-зинов, на агрегацию тромбоцитов человека in vitro. Все изученные 1,3,4-тиадиазины оказывали антиагрегационный эффект и ингибировали агрегацию, индуцированную как аденозиндифосфор-ной кислотой (АДФ), так и арахидоновой кислотой, в широком диапазоне концентраций. Наиболее активными соединениями среди всех изученных 1,3,4-тиадиазинов являются L-19, L-20, L-25, L-28 и L-31, эффективно снижающие агрегацию тромбоцитов, индуцированную арахидоновой кислотой и АДФ, в концентрациях 0,01-1 мм |
P 72 Platelet aggregation inhibitor properties of 1,3,4-thiadiazine thiadiazines [Text] / T. M. Vasilyeva, V. A. Makarov, O. N. Chupakhin, L. P. Sidorova, N. M. Perova, V. L. Rusinov // Gematologiya i Transfusiologiya . - 2008. - Vol. 53, № 4. - P12-15. - Bibliogr. : p. 15 (14 ref.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): 1,3,4-THIADIAZINES -- PLATELET AGGREGATION -- ARACHIDONIC ACID -- ADP Аннотация: Effects of new 1,3,4-thiadiazines on human platelet aggregation were studied in vitro. All 1,3,4-thiadiazines inhibited aggregation induced by ADP and arachidonic acid in a wide range of concentrations. The most active of the studied 1,3,4-thiadiazines were L-19, L-20, L-25, L-28, and L-31 in concentrations of 0.01-1 mM, effectively reducing platelet aggregation induced by arachidonic acid and ADP. |
В 58 Влияние новых соединений класса 1,3,4-тиадиазинов на агрегацию тромбоцитов in vitro и ex vivo [] = Influence of new 1,3,4-thiadiazines on platelet aggregation in vitro and ex vivo / Ю. С. Логвинова, Т. М. Васильева, В. А. Макаров, О. Н. Чупахин, Л. П. Сидорова, Н. М. Перова, В. Л. Русинов // Экспериментальная и клиническая фармакология. - 2010. - Т. 73, № 8. - С. 21-25 : рис., табл. - Библиогр.: с. 25 (13 назв.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: Исследовано влияние ряда новых оригинальных 4'-хлорфенил-, 4'-бромфенил-, 4'-фторфенил-1,3,4-тиадиазинов на агрегацию тромбоцитов человека in vitro. Все изученные 1,3,4-тиадиазины снижали агрегацию тромбоцитов, индуцированную как АДФ, так и арахидоновой кислотой. Наиболее активными соединениями являлись L-19, H-30, L-37. Исследовали также влияние внутривенного введения различных доз L-19 на агрегацию тромбоцитов и некоторые параметры плазменного гемостаза ex vivo |
С 38 Синтез и антиагрегационная активность 2-циклоалкиламино-5-тиенил- и 5-фурил-6H-1,3,4-тиадиазинов [] = Synthesis and antiaggregant activity of 2-cycloalkylamino-5-thienyl and 5-furyl-6H-1,3,4-thiadiazines / О. Н. Чупахин, Л. П. Сидорова, Н. М. Перова, В. Л. Русинов, Т. М. Васильева, В. А. Макаров // Химико-фармацевтический журнал. - 2011. - Т. 45. № 5. - С. 12-17 : граф., табл. - Библиогр.: с. 16 (12 назв.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: Синтезирована серия новых 5-(тиенил-2)-, 5-(фурил-2)- и 5-(тиенил-3)-замещенных 1,3,4-тиадиазинов циклоконденсацией ?-бромацетилтиофенов или ?-бром-2-ацетилфурана с 4-замещенными тиосемикарбазидами и изучена их антиагрегационная активность in vitro на тромбоцитах крови человека и ex vivo - на кроликах. Наиболее активные 5-(тиенил-2)-замещенные 1,3,4-тиадиазины ингибировали индуцированную АДФ и арахидоновой кислотой агрегацию тромбоцитов крови человека в широком интервале концентраций, что позволяет рассматривать их как потенциальные лекарства скорой помощи для лечения и профилактики инфарктов и инсультов. |
6-Polyfluoroalkylated 2-thiouracils in the synthesis of pyrimido[2,1-b][1,3,5]thiadiazines by the double Mannich reaction [Electronic resource] / O. G. Khudina, A. E. Ivanova, Ya. V. Burgart, V. I. Saloutin, M. A. Kravchenko // Journal of Fluorine Chemistry. - 2013. - Vol.147. - P31-35 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): ALIPHATIC AND AROMATIC AMINES -- ETHYLENEDIAMINE -- FORMALDEHYDE Аннотация: 6-Polyfluoroalkyl-2-thiouracils react with formaldehyde and primary amines in EtOH (MeCN) at 2-mercapto and 3-amino groups to yield pyrimido[2,1-b][1,3,5] thiadiazines via the multicomponent double Mannich reaction. The structure of 3-benzyl-8-nonafluorobutyl-3,4-dihydro-2H,6H-pyrimido[2,1-b][1,3,5] thiadiazin-6-one was studied by the X-ray diffraction analysis. The use of ethylenediamine in these reactions yields 3,3′-ethane-1,2-diyl- bis(pyrimido[2,1-b]thiadiazinone) as a result of the bis-double Mannich cyclocondensation. 8-Polyfluoroalkyl-pyrimido[2,1-b]thiadiazines exhibit weak tuberculostatic activity \\\\Expert2\\NBO\\Journal of Fluorine Chemistry\\2013, v. 147, p.31.pdf |
F 70 Fluorinated 2-amino-5-phenyl-1,3,4-thiadiazines: synthesis and structures [Electronic resource] / E. V. Shchegol'kov, Ya. V. Burgart, V. I. Saloutin, O. N. Chupakhin // Russian Chemical Bulletin (Translation of Izvestiya Akademii Nauk, Seriya Khimicheskaya). - 2013. - Vol.62, №1. - С. 220-222 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): THIADIAZINES -- TAUTOMERIC STRUCTURES -- 4H-TAUTOMER Аннотация: Fluorinated 2-amino-5-phenyl-1,3,4-thiadiazines were obtained for the first time. A study of their tautomeric structures revealed that trifluoromethyl-containing 1,3,4-thiadiazines exist as the 4H-tautomer in both solutions and the solid state, while their monofluoroaryl analogs exist as the 6H-tautomer \\\\expert2\\nbo\\Russian Chemical Bulletin\\2013, 62 (2), 521-528.pdf |
I-60 Influence of a biologically active compound from substituted thiadiazines on transaminase activity in myocardial homogenate in experimental myocardial infarction [Electronic resource] / O. N. Chupakhin, A. Sarapultsev, M. Chereshneva, I. Gette, L. P. Sidorova, I. Danilova, P. Sarapultsev // International Journal of Pharmacy and Pharmaceutical Sciences. - 2015. - Vol. 7, № 6. - С. 147-151. - Bibliogr. : p. 151 (21 ref.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): ENZYMES -- MYOCARDIAL INFARCTION -- L-17 COMPOUND Аннотация: Objective: Earlier works have reported on the effectiveness of the compounds of the group of substituted 5R1, 6R2, 3,4-thiadiasine-2-amines for treating experimental myocardial infarction, conditioned by the immune-modifying action of the compound. The purpose of this study was to evaluate the action of the L17 compound of the group of substituted 5R1, 6R2, 3,4-thiadiasine-2-amines on the extent of injury and the possible recurrence of experimental myocardial infarction by the dynamic assessment of transaminase activity in blood and myocardial homogenate (tissue). Methods: Modelling of myocardial infarction in rats was performed in accordance with the author’s modification of the standard ligation model. Tissue enzyme activity of LDH and CK-MB was evaluated at days 1, 7, and 14. Results: According to the results, the decrease in LDH 1-2 activity in tissue (after experimental myocardial infarction) corresponded to the increase in enzyme activity in blood on the first day of the experiment. However, on the seventh day of the experiment, the decrease of LDH 1-2 activities in the tissue of animals treated with L17 compound corresponded with the decrease of LDH activity in blood, while in non-treated animals the relation between the enzyme levels in blood and tissue was typical for the onset of MI. Conclusions: The evaluation of enzyme levels in myocardial tissue confirms previouslyreported data that the administration of a thiadiazine compounds prevents the recurrence and decreases the size of experimental myocardial infarction. \\\\expert2\\nbo\\International Journal of Pharmacy and Pharmaceutical Sciences\\52015. V. 7, N 6. P. 147-151.pdf |
S 98 Synthesis of New 1,3,4-Thiadiazines Capable of Inhibiting Nonenzymatic Glycosylation of Proteins [Electronic resource] / L. P. Sidorova, T. A. Tseitler, N. M. Perova, V. V. Emel’yanov, E. A. Savateeva, N. E. Maksimova, N. N. Mochul’skaya, V. A. Chereshnev, O. N. Chupakhin // Pharmaceutical Chemistry Journal. - 2015. - Vol. 49, № 8. - С. 501-505. - Bibliogr. : p. 505 (12 ref.) Рубрики: ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): 1,3,4-THIADIAZINE -- CYCLOCONDENSATION -- NONENZYMATIC GLYCOSYLATION OF PROTEINS -- THIOSEMICARBAZIDES Аннотация: A series of new 1,3,4-thiadiazines with cycloalkylamino (cyclopropylamino, cyclobutylamino, cyclopentylamino, cyclohexylamino) groups were synthesized via cyclocondensation of α-haloacetophenones with thiosemicarbazides containing 4-cycloalkyl groups. Five of the synthesized compounds showed the capability to inhibit nonenzymatic glycosylation of proteins in vitro in a model system. The obtained test results allowed compounds containing cyclopropylamino residues (LT-1a and LT-1d) to be recommended for further in vivo testing \\\\expert2\\nbo\\Pharmaceutical Chemistry Journal\\2015, 49 (8), 501-505.pdf |
T 44 The impact of immunomodulator compound from the group of substituted thiadiazines on the course of stress reaction [Electronic resource] / P. Sarapultsev, O. N. Chupakhin, S. Medvedeva, E. A. Mukhlynina, S. A. Brilliant, L. P. Sidorova, I. Danilova, A. Sarapultsev // International Immunopharmacology. - 2015. - Vol. 25, № 2. - С. 440-449. - Bibliogr. : p. 447-449 (101 ref) Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): STRESS -- THIADIAZINES -- L-17 COMPOUND Аннотация: A significant role of the stress response to many different diseases prompted a search for new specialized and non-specialized anti-stress agents. This study examines the effect of the compound L17 from the group of 5-phenyl substituted-6H-1,3,4-thiadiazine-2-amines, on the manifestations of the stress response. The authors used a standard model of immobilization stress, in which an animal was immobilized on its back for 6 ha day. Parameters of the morphological and functional states of the organs studied were measured and biochemical and enzyme-immunoassays were carried out on the first and second days. This study reveals that the main mechanism by which the L17 compound mediates of its anti-stress was by activation of macrophages on the second day of the experiments and the inhibition of apoptosis in the thymus. The results enable us to suggest that the compound L17 does not improve resistance to stress; however, it does lower the reaction to stress. \\\\expert2\\nbo\\International Immunopharmacology\\2015. V. 25, N 2. P. 440-449.pdf |
E 27 Effects of a compound from the group of substituted thiadiazines with hypothermia inducing properties on brain metabolism in rats, a study in vivo and in vitro / O. B. Shevelev, N. B. ILLARIONOVA, D. V. Petrovski, A. P. Sarapultsev, O. N. Chupakhin, M. P. Moshkin // PLOS ONE . - 2017. - Vol. 12, № 7. - С. е0180739[1-12] Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): ГИПОТЕРМИЯ -- HYPOTHERMIA -- 1,3,4-THIADIAZINE -- МЕТАБОЛИТЫ МОЗГА -- BRAIN METABOLITES -- ТЕРМОРЕГУЛЯЦИЯ -- THERMOREGULATION Аннотация: The aim of the present study was to examine how administration of a compound of 1,3,4-thiadiazine class 2-morpholino-5-phenyl-6H-1,3,4-thiadiazine, hydrobromide (L-17) with hypothermia inducing properties affects the brain metabolism. The mechanism by which L-17 induces hypothermia is unknown; it may involve hypothalamic central thermoregulation as well as act via inhibition of energy metabolism. We tested the hypothesis that L-17 may induce hypothermia by directly inhibiting energy metabolism. The study in vivo was carried out on Sprague-Dawley adult rats. Two doses of L-17 were administered (190 mg/ kg and 760 mg/kg). Brain metabolites were analyzed in control and treated groups using magnetic resonance spectroscopy, along with blood flow rate measurements in carotid arteries and body temperature measurements. Further in vitro studies on primary cultures from rat hippocampus were carried out to perform a mitochondria function test of L-17 preincubation (100 μM, 30 min). Analysis of brain metabolites showed no significant changes in 190 mg/kg treated group along with a significant reduction in body temperature by 1.5ÊC. However, administration of L-17 in higher dose 760 mg/kg provoked changes in brain metabolites indicative of neurotoxicity as well as reduction in carotid arteries flow rate. In addition, a balance change of excitatory and inhibitory neurotransmitters was observed. The L-17 pre-incubation with cell primary cultures from rat brain showed no significant changes in mitochondrial function. The results obtained in the study indicate that acute administration of L-17 190 mg/kg in rats induces mild hypothermia with no adverse effects onto brain metabolism. \\\\Expert2\\NBO\\PLoS ONE\\2017 V. 12 N 7 p. e0180739.pdf |
Immunomodulatory action of substituted 1,3,4-thiadiazines on the course of myocardial infarction / A. P. Sarapultsev, P. A. Sarapultsev, L. R. Ianalieva, O. N. Chupakhin, L. P. Sidorova, P. M. Vassiliev // Molecules. - 2018. - Vol. 23, № 7. - P1611 Рубрики: ХИМИЧЕСКИЕ НАУКИ |
T 89 Tseitler, T. A. 5-thienyl-2-cycloalkylamino-1,3,4-thiadiazines, hydrobromides / T. A. Tseitler, L. P. Sidorova, O. N. Chupakhin // Современные синтетические методологии для создания лекарственных препаратов и функциональных материалов (MOSM2018): вторая международная научно-практическая конференция : материалы и доклады. - Екатеринбург, 2019. - С. 109 Рубрики: ХИМИЧЕСКИЕ НАУКИ |