IN VITRO ПРОТИВОТУБЕРКУЛЕЗНАЯ И ПРОТИВОДИАБЕТИЧЕСКАЯ АКТИВНОСТЬ О-ТОЗИЛАТОВ-β-АМИНОПРОПИОАМИДОКСИМОВ И ХЛОРИДОВ 2-(ГЕТЕРОАМИНО)-1,5-ДИАЗАСПИРО[4,5]ДЕКАН-1- ЕН-5-АММОНИУМОВ

O-Tosylates-β-aminopropioamidoximes and chlorides of 2-amino-4,5-dihydrospyropyrazolylammoniums have been studied in vitro for anti-tuberculosis and anti-diabetic activity. In two groups of compounds containing β-amino groups: piperidin-1-yl, morpholin-1-yl, thiomorpholin-1-yl, 4-phenylpiperazine-1-yl, benzimidazol-1-yl (with the exception of the benzimidazole derivative in the spiro derivative series), drugs with an average anti-tuberculosis activity were detected on the DS strains of M. tuberculosis (MBC 50 μg/ml) and with moderate anti-diabetic α-amylase activity (27% to 29%) in the first row, containing β-amino groups: piperidin-1-yl, morpholin-1-yl and in the second row – piperidin-1-yl. References [1] Singh A., Prasad R., Balasubramanian V., Gupta N., Gupta P. Prevalence of adverse drug reaction with first-line drugs among patients treated for pulmonary tuberculosis // Clinical epidemiology and global health. 2015. Vol. 3. P. 80-90. [2] Yang T.W., Park H.O., Jang H.N., Yang J.H., Kim S.H., Moon S.H., Byun J.H., Lee C.E., Kim J.W., Kang D.H. Side effects associated with the treatment of multidrug-resistant tuberculosis at a tuberculosis referral hospital in South Korea: A retrospective study // Medicine. 2017. Vol. 96, Issue 28. e7482. [3] Forouhi N.G. and Wareham N.J. Epidemiology of diabetes // Medicine (Abingdon). 2014. Vol. 42, N 12. Р. 698-702. [4] Williams textbook of endocrinology (12th ed.). Philadelphia: Elsevier/Saunders. P. 13711435. ISBN 978-1-4377-0324-5. [5] Australian Indigenous HealthInfoNet, Chronic conditions: Diabetes. Accessed 31 August 2016. [6] Zaklyuchitel'nyy otchet po proektu KN MON RK «Proizvodnye β-aminopropioamidoksimov kak novye, netoksichnye i aktivnye tuberkulostatiki», 2003 g. Inv. nomer № 0203 RK 00809. P. 57-62. [7] Patent RK № 32421. Primenenie gidrohlorida O-para-toluoil-β-(morfolin-1-il)propioamidoksima v kachestve protivodiabeticheskogo sredstva / Kayukova L.A., Praliev K.D., Dyusembaeva G.T., Gulyaev A.E., Shul'gau Z.T., Sergazy Sh.D., Nurgozhin T.S.; opubl. 16.10.2017, Byul. №10. [8] Baytursynova G.P., Kayukova L.A., Geronikaki A., Praliev K.D., Kenesbekova A.K. Cintez O-para-toluolsul'fonil-β-aminopropioamidoksimov // Himicheskiy zhurnal Kazahstana. 2016. N 4. P. 114-122. [9] Kayukova L.A., Baytursynova G.P., Geronikaki A., Praliev K.D., Akatan K., Shaymor- dan E., Kaynarbaeva Zh.N. Tozilaty β-aminopropioamidoksimov v usloviyah otschepleniya uhodyaschey gruppy // Himicheskiy zhurnal Kazahstana. 2016. N 4. P. 328-335. [10] Mashkovskiy D.M. Lekarstvennye sredstv. 14-e izdanie. M.: Novaya volna, 2002. Vol. 2. P. 273-288. [11] Doulou I., Kontogiorgis C., Koumbis A.E., Evgenidou E., Hadjipavlou-Litina D., Fylaktakidou C. Synthesis of stable aromatic and heteroaromatic sulfonyl-amidoximes and evaluation of their antioxidant and lipid peroxidation activity // European Journal of Medicinal Chemistry. 2014. N 80. P. 145-153. [12] Bernfeld P. // in: Methods in Enzymology, Colowick S. P. and Kaplan N. O. (eds.). NewYork: Academic Press, 1955. P. 149-158.