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New triazinoindole bearing thiazole/oxazole analogues: Synthesis, α-amylase inhibitory potential and molecular docking study.
Rahim, Fazal; Tariq, Sundas; Taha, Muhammad; Ullah, Hayat; Zaman, Khalid; Uddin, Imad; Wadood, Abdul; Khan, Aftab Ahmad; Rehman, Ashfaq Ur; Uddin, Nizam; Zafar, Salman; Shah, Syed Adnan Ali.
  • Rahim F; Department of Chemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan. Electronic address: fazalstar@gmail.com.
  • Tariq S; Department of Chemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan.
  • Taha M; Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia. Electronic address: mtaha@iau.edu.sa.
  • Ullah H; Department of Chemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan.
  • Zaman K; Department of Chemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan.
  • Uddin I; Department of Chemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan.
  • Wadood A; Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan.
  • Khan AA; Department of Chemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan.
  • Rehman AU; Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan.
  • Uddin N; Department of Chemistry, University of Karachi, Karachi 75270, Pakistan.
  • Zafar S; Institute of Chemical Science, University of Peshawar, Khyber Pakhtunkhwa, Pakistan.
  • Shah SAA; Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Universiti Teknologi MARA Cawangan Selangor Kampus Puncak Alam, 42300 Bandar Puncak Alam, Selangor D.E., Malaysia; Faculty of Pharmacy, Universiti Teknologi MARA Cawangan Selangor Kampus Puncak Alam, 42300 Bandar Puncak Alam, Selangor
Bioorg Chem ; 92: 103284, 2019 11.
Article en En | MEDLINE | ID: mdl-31546207
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 ±â€¯0.20, 1.90 ±â€¯0.30, 1.2 ±â€¯0.30, 1.2 ±â€¯0.01 and 1.30 ±â€¯0.20 µM respectively, showed excellent α-amylase inhibitory potential when compared with acarbose as standard (IC50 = 0.91 ±â€¯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.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Oxazoles / Tiazoles / Triazinas / Alfa-Amilasas / Simulación del Acoplamiento Molecular / Inhibidores de Glicósido Hidrolasas Límite: Humans Idioma: En Año: 2019 Tipo del documento: Article

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Oxazoles / Tiazoles / Triazinas / Alfa-Amilasas / Simulación del Acoplamiento Molecular / Inhibidores de Glicósido Hidrolasas Límite: Humans Idioma: En Año: 2019 Tipo del documento: Article