Development of diarylpentadienone analogues as alpha-glucosidase inhibitor: Synthesis, in vitro biological and in vivo toxicity evaluations, and molecular docking analysis

• Main Authors: Maryam Aisyah, Abdullah, Lee, Yu-Ri, Siti Nurulhuda, Mastuki, Leong, Sze Wei, Wan Norhamidah, Wan Ibrahim, Muhammad Alif, Mohammad Latif, Aizi Nor Mazila, Ramli, Mohd F. F., Mohd Aluwi, Siti Munirah, Mohd Faudzi, Kim, Cheol-Hee
• Format: Article
• Language: English; English
• Published: Academic Press Inc. 2020
• Subjects: TP Chemical technology
• Online Access: http://umpir.ump.edu.my/id/eprint/30212/1/Development%20of%20diarylpentadienone%20analogues%20as%20alpha-glucosidase%20inhibitor.pdf; http://umpir.ump.edu.my/id/eprint/30212/2/Development%20of%20diarylpentadienone%20analogues%20as%20alpha-glucosidase%20inhibitor_FULL.pdf; http://umpir.ump.edu.my/id/eprint/30212/; https://doi.org/10.1016/j.bioorg.2020.104277; https://doi.org/10.1016/j.bioorg.2020.104277
• Institution: Universiti Malaysia Pahang

A series of aminated- (1–9) and sulfonamide-containing diarylpentadienones (10–18) were synthesized, structurally characterized, and evaluated for their in vitro anti-diabetic potential on α-glucosidase and DPP-4 enzymes. It was found that all the new molecules were nonassociated PAINS compounds. Th...