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- Title
α-Glucosidase inhibitory potential and hemolytic evaluation of newly synthesized 3,4,5-trisubstituted-1,2,4-triazole derivatives.
- Authors
Nafeesa, Khadija; Aziz-ur-Rehman; Abbasi, Muhammad Athar; Siddiqui, Sabahat Zahra; Rasool, Shahid; Ali Shah, Syed Adnan; Ashraf, Muhammad; Jahan, Bakhat; Lodhi, Muhammad Arif; Khan, Farman Ali
- 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, 13C-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.
- Subjects
APROTIC solvents; GLUCOSIDASES; AROMATIC amines; CHLORIDES
- Publication
Pakistan Journal of Pharmaceutical Sciences, 2019, Vol 32, Issue 6, p2651
- ISSN
1011-601X
- Publication type
Article