Synthesis and novel structural hybrid analogs of oxindole derivatives bearing piperidine ring, their antidiabetics II activity and molecular docking study

Synthesis of new potent antidiabetic scaffolds have grabbed the attention of researchers worldwide. In this context, new oxindole bearing piperidine derivatives (1–18) were synthesized and characterized using 1 HNMR, 13CNMR, and EI-MS, and then tested their potency as α-glucosidase and α-amylase inh...

詳細記述

書誌詳細
出版年:Journal of Molecular Structure
第一著者: Mukhliss L.; Taha M.; Rahim F.; Adalat B.; Ajmal A.; Wadood A.; Uddin N.; Khan K.M.; Ali Shah S.A.
フォーマット: 論文
言語:English
出版事項: Elsevier B.V. 2025
オンライン・アクセス:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85217236617&doi=10.1016%2fj.molstruc.2025.141666&partnerID=40&md5=864bca5fc5b352439f5852004ab8b3a4
その他の書誌記述
要約:Synthesis of new potent antidiabetic scaffolds have grabbed the attention of researchers worldwide. In this context, new oxindole bearing piperidine derivatives (1–18) were synthesized and characterized using 1 HNMR, 13CNMR, and EI-MS, and then tested their potency as α-glucosidase and α-amylase inhibitors. When compared to the standard inhibitor acarbose, which has an IC50 value of 10 0.30 ± 0.20µM for α-amylase and 9.80 ± 0.20 µM for α-glucosidase, all the compounds in the series showed exceptional α-amylase and α-glucosidase inhibition. The most effective derivative in the series is derivative 8 with an IC50 value of 0.30 ± 0.05 µM for α-amylase and 0.40 ± 0.05 µM for α-glucosidase, which is significantly more effective than the common acarbose. Structure-activity relationship (SAR) was established based on the alteration of position of the substituents on the phenyl portion. The most effective drugs' binding interactions were studied using molecular docking techniques. © 2025 Elsevier B.V.
ISSN:222860
DOI:10.1016/j.molstruc.2025.141666