| Literature DB >> 31546207 |
Fazal Rahim1, Sundas Tariq2, Muhammad Taha3, Hayat Ullah2, Khalid Zaman2, Imad Uddin2, Abdul Wadood4, Aftab Ahmad Khan2, Ashfaq Ur Rehman4, Nizam Uddin5, Salman Zafar6, Syed Adnan Ali Shah7.
Abstract
New triazinoindole bearing thiazole/oxazole analogues (1-21) were synthesized and characterized through spectroscopic techniques such as HREI-MS, 1H and 13C NMR. The configuration of compound 2i and 2k was confirmed through NOESY. All analogues were evaluated against α-amylase inhibitory potential. Among the synthesized analogues, compound 1h, 1i, 1j, 2a and 2f having IC50 values 1.80 ± 0.20, 1.90 ± 0.30, 1.2 ± 0.30, 1.2 ± 0.01 and 1.30 ± 0.20 μM respectively, showed excellent α-amylase inhibitory potential when compared with acarbose as standard (IC50 = 0.91 ± 0.20 µM). All other analogues showed good to moderate inhibitory potential. Structural activity relationship (SAR) has been established and binding interactions were confirmed through docking studies.Entities:
Keywords: Molecular docking; Oxazole; SAR; Synthesis; Thiazole; Triazinoindole; α-amylase
Year: 2019 PMID: 31546207 DOI: 10.1016/j.bioorg.2019.103284
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275