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

• 出版年: JOURNAL OF MOLECULAR STRUCTURE
• 主要な著者: Mukhliss, Layan; Taha, Muhammad; Rahim, Fazal; Adalat, Bushra; Ajmal, Amar; Wadood, Abdul; Uddin, Nizam; Khan, Khalid Mohammed; Shah, Syed Adnan Ali
• フォーマット: 論文
• 言語: English
• 出版事項: ELSEVIER 2025
• 主題: Chemistry
• オンライン･アクセス: https://www-webofscience-com.uitm.idm.oclc.org/wos/woscc/full-record/WOS:001426238300001
• ISSN: 0022-2860; 1872-8014
• DOI: 10.1016/j.molstruc.2025.141666

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 alpha-glucosidase and alpha-amylase inhibitors. When compared to the standard inhibitor acarbose, which has an IC50 value of 10 0.30 f 0.20 mu M for alpha-amylase and 9.80 f 0.20 mu M for alpha-glucosidase, all the compounds in the series showed exceptional alpha-amylase and alpha-glucosidase inhibition. The most effective derivative in the series is derivative 8 with an IC50 value of 0.30 f 0.05 mu M for alpha-amylase and 0.40 f 0.05 mu M for alpha-glucosidase, which is significantly more effective than the common acarbose. Structureactivity 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.