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  • Küçük Resim
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    NMR study of the inclusion complexes of beta-cyclodextrin with diphenhydramine, clonidine and tolperisone
    (Springer International Publishing AG, 2022) Zhumakova, Symbat; Ten, Assel; Zharkynbek, Tolganay; Yu, Valentina; Seilkhanov, Tulegen; Basharimova, Anna; Bayazit, Sarah; Aydemir, Murat; Zazybin, Alexey
    Forming complexes with beta-cyclodextrin can enhance stability, dissolution rate, solubility, and bioavailability of an active pharmaceutical ingredient. In this study, the inclusion behavior between beta-cyclodextrin (beta-CD) and diphenhydramine, clonidine, and tolperisone in DMSO-d(6) was investigated using NMR spectroscopy. H-1, C-13, COSY, HMQC, and ROESY data were applied to determine the structure of inclusion complexes, and molecular docking analysis was engaged to identify the most favorable host-guest interactions in the inclusion complexes. Complexation of beta-CD with diphenhydramine, clonidine, and tolperisone is accompanied by the insertion of a molecular fragment of the guest molecule, one molecule of diphenhydramine and tolperisone, and two molecules of clonidine, into the inner sphere of one host molecule. The reported study provides useful information for the potential application of the complexation of beta-CD with diphenhy-dramine, clonidine, and tolperisone. This may be a good strategy for the development of solid pharmaceutical dosage forms based on beta-CDs as a drug delivery system.
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    Ultrasound- and microwave-promoted synthesis, growth-regulating activity and antimicrobial behavior of trimecaine-based Ionic compounds
    (Wiley-V C H Verlag Gmbh, 2022) Dauletbakov, Anuar; Zazybin, Alexey; Yu, Valentina; Belyankova, Yelizaveta; Ten, Assel; Rafikova, Khadichakhan; Zolotareva, Darya; Aydemir, Murat
    The present work describes the synthesis, growth-regulating activity, and antimicrobial behavior of ionic compounds based on 2-diethylamino-N-(2,4,6-trimethylphenyl)acetamide (trimecaine). Synthesis of ionic compounds was performed via N-alkylation of trimecaine with alkyl halides using microwave and ultrasound activation and the results were compared with those of classical conditions (thermal activation). The synthesized ionic compounds have been tested for germination energy and capacity with the collection of different varieties and hybrids of sweet sorghum seeds. The valuable results were obtained for the seeds stored for several years for which the significant drop in germination activity is usually observed. Furthermore, the ionic compounds were used to study their biological activity - growth -regulating activity on sweet sorghum seeds and the antimicrobial behavior against E. coli, S. typhimurium, B. subtilis, S. aureus, P. aeruginosa, and C. albicans microorganisms.