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]

Author(s):

1. Khadija Nafeesa: Department of Chemistry, GC University,Lahore,Pakistan

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

3. Muhammad Athar Abbasi: Department of Chemistry, GC University,Lahore,Pakistan

4. Sabahat Zahra Siddiqui: Department of Chemistry, GC University,Lahore,Pakistan

5. Shahid Rasool: Department of Chemistry, GC University,Lahore,Pakistan

6. 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

7. Muhammad Ashraf: Department of Chemistry, The Islamia University of Bahawalpur,Bahawalpur,Pakistan

8. Bakhat Jahan: Department of Chemistry, The Islamia University of Bahawalpur,Bahawalpur,Pakistan

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

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

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

Page(s): 2651-2658

DOI: DOI not available

Published: Journal: Pakistan Journal of Pharmaceutical Sciences, Volume: 32, Issue: 6, Year: 2019

Keywords:

sulfonamides , hemolytic activity , anti aglucosidase , 4Triazoles

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