New triazinoindole bearing thiazole/oxazole analogues: Synthesis, α-amylase inhibitory potential and molecular docking study.
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⯵M respectively, showed excellent α-amylase inhibitory potential when compared with acarbose as standard (IC50â¯=â¯0.91⯱â¯0.20⯵M). All other analogues showed good to moderate inhibitory potential. Structural activity relationship (SAR) has been established and binding interactions were confirmed through docking studies.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Oxazoles
/
Tiazoles
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Triazinas
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Alfa-Amilasas
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Simulación del Acoplamiento Molecular
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Inhibidores de Glicósido Hidrolasas
Límite:
Humans
Idioma:
En
Año:
2019
Tipo del documento:
Article