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α-Glucosidase inhibitory potential and hemolytic evaluation of newly synthesized 3,4,5-trisubstituted-1,2,4-triazole derivatives.
- Source :
- Pakistan Journal of Pharmaceutical Sciences; Nov2019, Vol. 32 Issue 6, p2651-2658, 8p
- Publication Year :
- 2019
-
Abstract
- A series of 1, 2, 4-triazole derivatives bearing piperidine moiety has been introduced as new anti-diabetic drug candidates with least cytotoxicity. p-Chlorophenylsulfonyl chloride (1) and ethyl nipecotate (2) were the starting reagents that resulted into corresponding 3,4,5-trisubstituted-1,2,4-triazole (6) through a series of steps. A series of electrophiles, 9a-e, were synthesized by reacting 4-bromobutyryl chloride (7) with differently substituted aromatic amines (8a-e) under basic aqueous medium. Target derivatives, 10a-e, were synthesized by the reaction of compound 6 with N-aryl-4-bromobutanamides (9a-e) in an aprotic solvent. Structures of all the derivatives were verified by spectroscopic analysis using IR, ¹H-NMR, <superscript>13</superscript>C-NMR and EIMS. Most of the derivatives revealed moderate to good α-glucosidase inhibitory activity with reference to acarbose. The moderate hemolytic potential demonstrated least toxicity. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 1011601X
- Volume :
- 32
- Issue :
- 6
- Database :
- Supplemental Index
- Journal :
- Pakistan Journal of Pharmaceutical Sciences
- Publication Type :
- Academic Journal
- Accession number :
- 139829903