Abstract
New antidiabetic agents are being sought because of the global problem with diabetes. Amidoxime derivatives are known to have antidiabetic activity. β-Aminopropionamidoxime bases and pharmacologically acceptable salts of O-aroyl-β-(morpholin-1-yl)propionamidoximes and 5-substituted phenyl-3-β-(piperidin-1-yl and morpholin-1-yl)ethyl-1,2,4-oxadiazoles were screened in vitro for antidiabetic activity manifested as inhibition of α-amylase and α-glucosidase. Compounds with pronounced antidiabetic properties were identified. The series of 3,5-disubstituted 1,2,4-oxadiazoles were more active than the series of O-aroyl-β-aminopropionamidoximes. The results could be used for further in vivo screening of the antidiabetic properties of the most promising compounds with a preliminary assessment of their mean toxic doses in animals.
| Original language | English |
|---|---|
| Pages (from-to) | 129-133 |
| Number of pages | 5 |
| Journal | Pharmaceutical Chemistry Journal |
| Volume | 53 |
| Issue number | 2 |
| DOIs | |
| Publication status | Published - May 5 2019 |
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Keywords
- bases and pharmacologically acceptable salts of O-aroyl-β-(morpholin-1-yl)propionamidoximes and 5-substituted phenyl-3-β-(piperidin-1-yl and morpholin-1-yl)ethyl-1,2,4-oxadiazoles
- in vitro antidiabetic screening for inhibition of α-amylase and α-glucosidase
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery
Cite this
Inhibition of α-Amylase and α-Glucosidase by New β-Aminopropionamidoxime Derivatives. / Kayukova, L. A.; Uzakova, A. B.; Baitursynova, G. P.; Dyusembaeva, G. T.; Shul’gau, Z. T.; Gulyayev, Alexander; Sergazy, Sh D.
In: Pharmaceutical Chemistry Journal, Vol. 53, No. 2, 05.05.2019, p. 129-133.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Inhibition of α-Amylase and α-Glucosidase by New β-Aminopropionamidoxime Derivatives
AU - Kayukova, L. A.
AU - Uzakova, A. B.
AU - Baitursynova, G. P.
AU - Dyusembaeva, G. T.
AU - Shul’gau, Z. T.
AU - Gulyayev, Alexander
AU - Sergazy, Sh D.
PY - 2019/5/5
Y1 - 2019/5/5
N2 - New antidiabetic agents are being sought because of the global problem with diabetes. Amidoxime derivatives are known to have antidiabetic activity. β-Aminopropionamidoxime bases and pharmacologically acceptable salts of O-aroyl-β-(morpholin-1-yl)propionamidoximes and 5-substituted phenyl-3-β-(piperidin-1-yl and morpholin-1-yl)ethyl-1,2,4-oxadiazoles were screened in vitro for antidiabetic activity manifested as inhibition of α-amylase and α-glucosidase. Compounds with pronounced antidiabetic properties were identified. The series of 3,5-disubstituted 1,2,4-oxadiazoles were more active than the series of O-aroyl-β-aminopropionamidoximes. The results could be used for further in vivo screening of the antidiabetic properties of the most promising compounds with a preliminary assessment of their mean toxic doses in animals.
AB - New antidiabetic agents are being sought because of the global problem with diabetes. Amidoxime derivatives are known to have antidiabetic activity. β-Aminopropionamidoxime bases and pharmacologically acceptable salts of O-aroyl-β-(morpholin-1-yl)propionamidoximes and 5-substituted phenyl-3-β-(piperidin-1-yl and morpholin-1-yl)ethyl-1,2,4-oxadiazoles were screened in vitro for antidiabetic activity manifested as inhibition of α-amylase and α-glucosidase. Compounds with pronounced antidiabetic properties were identified. The series of 3,5-disubstituted 1,2,4-oxadiazoles were more active than the series of O-aroyl-β-aminopropionamidoximes. The results could be used for further in vivo screening of the antidiabetic properties of the most promising compounds with a preliminary assessment of their mean toxic doses in animals.
KW - bases and pharmacologically acceptable salts of O-aroyl-β-(morpholin-1-yl)propionamidoximes and 5-substituted phenyl-3-β-(piperidin-1-yl and morpholin-1-yl)ethyl-1,2,4-oxadiazoles
KW - in vitro antidiabetic screening for inhibition of α-amylase and α-glucosidase
UR - http://www.scopus.com/inward/record.url?scp=85067354508&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85067354508&partnerID=8YFLogxK
U2 - 10.1007/s11094-019-01966-5
DO - 10.1007/s11094-019-01966-5
M3 - Article
VL - 53
SP - 129
EP - 133
JO - Pharmaceutical Chemistry Journal
JF - Pharmaceutical Chemistry Journal
SN - 0091-150X
IS - 2
ER -