Α-Glucosidase inhibitory potential and hemolytic evaluation of newly synthesized 3, 4, 5-trisubstituted-1, 2, 4-triazole derivatives | Pakistan Journal of Pharmaceutical Sciences 2019

Khadija Nafeesa Department of Chemistry, GC University,Lahore,Pakistan

Aziz-ur-Rehman Department of Chemistry, GC University,Lahore,Pakistan

Muhammad Athar Abbasi Department of Chemistry, GC University,Lahore,Pakistan

Sabahat Zahra Siddiqui Department of Chemistry, GC University,Lahore,Pakistan

Shahid Rasool Department of Chemistry, GC University,Lahore,Pakistan

Syed Adnan Ali Shah Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Universiti Teknologi MARA, Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia; Department of Pharmacy, Universiti Teknologi MARA, Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia

Muhammad Ashraf Department of Chemistry, The Islamia University of Bahawalpur,Bahawalpur,Pakistan

Bakhat Jahan Department of Chemistry, The Islamia University of Bahawalpur,Bahawalpur,Pakistan

Muhammad Arif Lodhi Department of Biochemistry, Abdul Wali Khan University,Mardan,Pakistan

Farman Ali Khan Department of Biochemistry, Abdul Wali Khan University,Mardan,Pakistan

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 aglucosidase inhibitory activity with reference to acarbose. The moderate hemolytic potential demonstrated least toxicity.