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1-(3-АМИНОПРОПИЛ)ИМИДАЗОЛ КАК ПРЕКУРСОР СТИМУЛЯТОРОВ РОСТА РАСТЕНИЙ
(2018-01-01)
Aigul Malmakova
;
V. К. Yu
;
P. Dauletbai
;
A. Dulatbaev
;
Kaldybay D. Praliyev
Novel imidazole derivatives had been synthesized. The possibility of using 1-(3aminopropyl)imidazole as a starting reagent is synthetically justified for the preparing of piperidone-4 with following conversion into a bicyclic ketone. The reduction of mono- and bicyclic ketones had been carried out under Kizner-Wolf reaction conditions to imidazole-containing piperidine and bispidine, whose β-cyclodextrin complexes stimulate the growth of agricultural plants. The composition and structure of the compounds are confirmed by elemental analysis, IR and 13C NMR spectra. References [1] Popov S.Ja. Dorozhkina L.A., Kalinin V.A. Osnovy himicheskoj zashhity rastenij / Pod red. professora S. Ja Popova. M.: Art-Lion, 2003. 208 P. [2] Tjuterev S.L. Himicheskie protraviteli. Protravlivanie semjan zernovyh kolosovyh kul'tur // Zashhita i karantin rastenij. 2005. P. 106-109. [3] Wahbi Y., Tournaire C., Caujolle R., Payard M., Linas M.D., Seguela J.P. Aliphatic ethers and esters of 1-(2,4-dichlorophenyl)-2-(IH-imidazolyl)ethanol: study of antifungal activity against yeasts and hydrophobic character // Eur. J. Med. Chem. 1994. 29. P. 701-706. [4] De Vita D., Scipione L., Tortorella S., Mellini P., Di Rienzo B., a Simonetti G., D'Auria F.D., Panella S., Cirilli R., Di Santo R., Palamara A.T. Synthesis and antifungal activity of a new series of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives // Eur. J. Med. Chem. 2012. 49. P. 334-342 [5] EP1675833A1. 1H-imidazole derivatives as cannabinoid receptor modulators / Josephus H.M. Lange, Cornelis G. Kruse Stuivenberg Herman H. VanHiskias G. Keizer. 2011-01-26. [6] WO 2005/095354 20051013. Proizvodnye imidazola, aktivnye v otnoshenii receptora SV1/ Cheng Lejfeng, Lindstedt-Al'stermark Jeva-Lotte, Boije Anna Marija Persdotter. 27.12.2009. [7] http://www.findpatent.ru/patent/235/2354650.html [8] https://www.eurolab.ua/medicine/atc/list/555/ [9] Yu V., Praliyev K., Nagimova A., Zazybin A. A simple one-pot synthesis of N-substituted 4-methyl-1-oxa-8-azaspiro[4,5]deca-3-en-3-carboxylic acids // Tetrahedron Letters. 2015. Vol. 56. P. 1631-1634. (Impact Factor: 2.39) (Scopus). [10] Yu V.K., Kabdraissova A.Zh., Praliyev K.D., Shin S.N., Berlin K.D. Synthesis and properties of novel alkoxy- and phenoxyalkyl ethers of secondary and tertiary ethynyl-piperdin-4ols possessing unusual analgesic, anti-bacterial, and anti-spasmotic activity as well as low toxicity //Journal of Saudi Chemical Society. 2009. 13. P. 209-217. [11] Pichkhadze G. M., Smagulova G.S., Kadyrova D.M., Praliev K.D., Yu V.K. Local Anesthetic Activity of a Promising Piperidine Derivative (LAS-54) in Combination with Epine-phrine // Pharmaceutical Chemistry Journal December 2016. Vol. 50, Issue 9. P. 600–602. DOI 10.1007/s11094-016-1498-7. IF 0,461. [12] Berlin K.D., Iskakova T.K., Faskhutdinov M.F., Praliyev K.D., Ch. P. Lee, Ten A Yu., Malmakova A. Unusual Conformational Behavior of 3,7-Dihetera(N,N-;N,O-;N,S-)bicyclo[3.3.1]nonan-9-ols in CDCl3 Phosphorus, Sulfur, and Silicon and the Related Elements. 2014. Vol. 189, N 7-8. P. 864-872. [13] Astahova A.V., Demina N.B. Sovremennye tehnologii lekarstvennyh form: poluchenie, issledovanie i primenenie kompleksov vkljuchenija lekarstvennyh veshhestv s ciklodekstrinami // Him.-farmac. zhurn. 2004. Vol. 38, N 2. P. 46-49. [14] Sharipov R.A. , Sharapov K.S., Kemelbekov U.S. , Volynkin V.A., Yu V.K., Panyushkin. The structure and pharmacological properties of the 4-acetoxy-1-(2-ethoxyethyl)-4-phenylpiperidine inclusion complex with β-cyclodextrin // Journal of Inclusion Phenomena and Macrocyclic Chemistry, 2016. 20 December. P. 1-8. DOI 10.1007/s10847-016-0685-1. [15] Tkachuk O.A., Pavlikova E.V., Orlov A.N. Jeffektivnost' primenenija reguljatorov rosta pri vozdelyvanii jarovoj pshenicy v uslovijah lesostepnoj zony Srednego Povolzh'ja // Molodoj uchenyj. 2013. N 4. P. 677-679.
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SYNTHESIS, STRUCTURE, AND BIOLOGICAL ACTIVITY OF NOVEL BISPIDINE DERIVATIVES
(Innovare Academic Sciences, 2021-01-31)
Aigul Malmakova
;
V. К. Yu
;
Kaldybay D. Praliyev
;
Altynay B. Kaldybayeva
;
М. К. Амиркулова
Objective: Derivatives of 3,7-diazabicyclo[3.3.1]nonan-9-one attract considerable attention from pharmacists for the treatment of a wide rangeof diseases. According to this interest, the novel derivatives of 3-cyclopropanmethyl-7-alkoxyalkyl-3,7-diazabicyclo[3.3.1]nonan-9-one withisopropoxypropyl and ethoxypropyl substituents in the position 7 had been synthesized to study their biological activity and toxicity. The practicalsignificance of the work is in the accumulation and development of scientific representations about diazabicyclic compounds, methods for theirsynthesis, structure, and properties, which can subsequently be used in a targeted design and identification of even more complex systems, as wellas in the development of further research in the field of 3,7-diazabicyclo[3.3.1]nonanes. For this purpose, complexes of the synthesized compoundswith β-cyclodextrin are obtained and their biological activity is investigated at the Department of Pharmacology of S.D. Asfendiyarov Kazakh NationalMedical University with the aid of the pharmacological tests.Methods: An experimental study of local anesthetic activity on the models of infiltration, conduction anesthesia, and acute toxicity of synthesizedmolecules was carried out using primary screening methods.Results: As a result of pharmacological screening, it has been found that the compounds exhibit local anesthetic activity and low toxicity and wasrecommended for in-depth study of their pharmacological properties.Conclusion: It turned out that a nature of the N-alkoxyalkyl radical does not affect the toxicity of cyclopropanmethyl- substituted bispidines. In theseries of O-benzoyloximes of bispidinones, the isopropoxypropyl- substituted analog is 1.3 times less toxic than ethoxypropyl- one.
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Hematopoietic and T-lymphopoiesis-stimulating effects of a fluorinated pyrazolopiperidine β-cyclodextrin complex in cyclophosphamide-induced hematopoietic suppression
(Frontiers Media, 2026-08-03)
Assel Yu. Ten
;
Lyailya Baktybayeva
;
Zhanargul Koshetova
;
Raushan B. Koizhaiganova
;
Guldana Daulet
Background Cyclophosphamide is widely used in oncology, autoimmune disorders, and transplantation-related conditioning or post-transplant immunosuppression. However, its therapeutic value is limited by hematopoietic and lymphoid toxicity, including leukopenia, neutropenia, anemia, thrombocytopenia, bone marrow suppression, thymic injury, and prolonged impairment of T-cell recovery. These effects may occur after pulsed intravenous administration, high-dose regimens used in transplantation or severe refractory disease, and continuous low-dose/metronomic exposure. Therefore, there is a medical need for pharmacological agents capable of compensating cyclophosphamide-induced hematopoietic and lymphopoietic suppression without causing uncontrolled stimulation of early progenitor cells. Aim To evaluate the hematopoietic and T-lymphopoiesis-stimulating activity of BIV under cyclophosphamide-induced hematopoietic and T-lymphopoietic suppression. Methods Cyclophosphamide-induced hematopoietic- and T-lymphopoiesis-suppressive models were established on laboratory albinos rats and C57BL6/J mice. Peripheral blood hematological indices in rats were measured using hematology analyzers. Hematopoietic stem cells, thymocyte subsets, Th act , T reg , T mem , CTL cell populations, and erythroid cells from the bone marrow, thymus, and spleen were analyzed by flow cytometry. Statistical analysis was performed using one-way ANOVA (p < 0.05). Results In rats with CPh-induced hematopoietic suppression, BIV supported partial recovery of erythrocyte and hemoglobin parameters and improved leukopoietic indices under CPh-induced hematopoietic suppression. The β-cyclodextrin complex of 5-benzyl-7-(o-fluorobenzylidene)-2,3-bis(o-fluorophenyl)-3,3a,4,5,6, 7-hexahydro-2H-pyrazolo[4,3-c]pyridine (BIV) demonstrated a consistent moderate activity in restoring the overall level of CD3ε+CD19− T lymphocytes in the bone marrow and thymus. In the bone marrow, BIV uniformly increased the reduced levels of CD3ε+CD19− T lymphocytes and CD3ε+CD44 + T mem memory T cells to physiological normal values. In the spleen, BIV restored the decreased levels of CD25+FoxP3+ T reg regulatory lymphocytes and CD28 + CD44 + T mem memory T cells to physiological normal levels, while reducing the elevated levels of CD3ε+CD8a+ CTL cytotoxic T lymphocytes and CD4 + CD25 + Th act activated helper T cells to values corresponding to the physiological norm. Conclusion BIV demonstrated notable hematopoietic- and T-lymphopoiesis-modulating activity. The compound partially restored erythropoiesis as well as central and peripheral T-lymphopoiesis, while providing balanced regulation of cytotoxic, regulatory, and memory T-cell subsets in cyclophosphamide-induced T-lymphopoiesis-suppressive models. Several evaluated T-lymphocyte subpopulations approached or returned to physiological control levels under the experimental conditions, although full translational validation requires further pharmacological and toxicological investigation.

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