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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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КЕЙБІР α-АМИНОФОСФОНАТТАР СИНТЕЗІ ЖӘНЕ БИОЛОГИЯЛЫҚ ҚАСИЕТТЕРІ
(2020-01-01)
Altynay B. Kaldybayeva
;
Aigul Malmakova
;
V. К. Yu
;
Kaldybay D. Praliyev
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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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Novel 7-Aryliden-3,3a,4,5,6,7-(hexahydro-5-(2-ethoxyethyl)-2-phenyl- 3-aryl-2H-pyrazolo[4,3-c]pyridine Hydrochloride: Synthesis and Structure
(2022-03-31)
Zh.A. Koshetova
;
V. К. Yu
;
Iskakova Tynyshtyk Kadyrovna
;
N. A. Zhumanova
;
Kayrat M. Beketov
A Claisen-Schmidt type reaction of 1-(2-ethoxyethyl)piperidin-4-one with different aromatic aldehydes led to corresponding dienones with a yield of 65‒71%. 7-Arylidene-3,3a,4,5,6,7-(hexahydro-5-(2-ethoxyethyl)-2-phenyl-3-aryl-2H-pyrazolo[4,3-c]pyridines were synthesized by heterocyclization of 3,5-diarylidene-piperidin-4-ones with phenylhydrazine hydrochloride in methanol at 70 °C over 4‒6 h. The X-ray crystal structure determination of 7-(p-methoxybenzyliden)-3,3a,4,5,6,7-(hexahydro-5-(2-ethoxyethyl)-2-phenyl-3-(p-methoxyphenyl)-2H-pyrazolo[4,3-c]pyridine hydrochloride (the deposition number is CCDC 862410) was completed. The piperidine and pyrazoline rings are close to a chair and envelope conformations, respectively.

Қазақ ұлттық қыздар педагогикалық университеті / Казахский национальный женский педагогический университет

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