Match!

New triazinoindole bearing thiazole/oxazole analogues: Synthesis, α-amylase inhibitory potential and molecular docking study

Published on Nov 1, 2019in Bioorganic Chemistry3.93
· DOI :10.1016/j.bioorg.2019.103284
Fazal Rahim25
Estimated H-index: 25
(HU: Hazara University),
Sundas Tariq (HU: Hazara University)+ 9 AuthorsSyed Adnan Ali Shah16
Estimated H-index: 16
(UiTM: Universiti Teknologi MARA)
Abstract
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.
  • References (19)
  • Citations (0)
References19
Newest
#1Nguyen Thi Luyen (VAST: Vietnam Academy of Science and Technology)H-Index: 4
#2Pham Thanh Binh (VAST: Vietnam Academy of Science and Technology)H-Index: 3
Last.Nguyen Phuong Thao (VAST: Vietnam Academy of Science and Technology)H-Index: 17
view all 7 authors...
4 CitationsSource
#1Roqia Bashary (Kabul University)H-Index: 1
#2Gopal L. Khatik (LPU: Lovely Professional University)H-Index: 9
4 CitationsSource
#2Taha MuhammadH-Index: 29
Last.Khalid Mohammed Khan (KU: University of Karachi)H-Index: 48
view all 10 authors...
6 CitationsSource
#1Hayat Ullah (HU: Hazara University)H-Index: 14
#2Fazal Rahim (HU: Hazara University)H-Index: 25
Last.Khalid Mohammed Khan (KU: University of Karachi)H-Index: 48
view all 10 authors...
11 CitationsSource
#1Taha Muhammad (UoD: University of Dammam)H-Index: 29
#2Muhammad Tariq Javid (HU: Hazara University)H-Index: 8
Last.Khalid Mohammed Khan (KU: University of Karachi)H-Index: 48
view all 10 authors...
14 CitationsSource
#1Farman Ali (KU: University of Karachi)H-Index: 6
#2Khalid Mohammed Khan (KU: University of Karachi)H-Index: 48
Last.Shahnaz PerveenH-Index: 27
view all 8 authors...
17 CitationsSource
#1Syahrul Imran (UiTM: Universiti Teknologi MARA)H-Index: 21
#2Taha Muhammad (UiTM: Universiti Teknologi MARA)H-Index: 29
Last.Jahidul Islam Mohammad (Cyberjaya University College of Medical Sciences)H-Index: 5
view all 6 authors...
11 CitationsSource
#1Taha Muhammad (UiTM: Universiti Teknologi MARA)H-Index: 29
#2Nor Hadiani Ismail (UiTM: Universiti Teknologi MARA)H-Index: 27
Last.Khalid Mohammed Khan (KU: University of Karachi)H-Index: 48
view all 9 authors...
22 CitationsSource
#1Fazal Rahim (HU: Hazara University)H-Index: 25
#2Muhammad Ali (CUI: COMSATS Institute of Information Technology)H-Index: 11
Last.Muhammad Bilal (CUI: COMSATS Institute of Information Technology)H-Index: 11
view all 11 authors...
17 CitationsSource
#1Fazal Rahim (HU: Hazara University)H-Index: 25
#2Muhammad Tariq Javed (HU: Hazara University)H-Index: 4
Last.Khalid Mohammed Khan (KU: University of Karachi)H-Index: 48
view all 11 authors...
28 CitationsSource
Cited By0
Newest