CD Skripsi
Sintesis, Uji Aktivitas Antidiabetes Dan Studi Molecular Docking Senyawa Piridazinon 6-(3-Bromofenil)-2-(Fenilsulfonil)Piridazin-3(2h)-On
Pyridazinone is oxo-pyridazine derivative compound that has broad bioactivity,
such as an analgesic, anti-inflammatory, antidiabetic, antihypertensive and
anticancer. For further development of pyridazinone compounds, in this study,
pyridazinone compound substituted benzenesulfonyl have been synthesized and
tested their activity as antidiabetic because the target molecule has a hydrophilic
group. Pyridazinone 6-(3-bromophenyl)-2-(phenylsulfonyl)pyridazine-3(2H)-one
was synthesized from 6-(3-bromophenyl)pyridazine-3(2H)-one through a
Claisent-Schmidt condensation reaction between 3-bromo acetophenone and
glyoxylic acid then a cyclization reaction occurs with hydrazine hydrate. The
pyridazinone compound formed is substituted with the benzensulfonyl chloride.
The structure of the synthesized compound was confirmed by characterization
using UV, FTIR, 1H-NMR and HRMS spectroscopy. Pyridazinone compounds
were tested for their antidiabetic activity through molecular docking and in vitro
studies. A molecular docking study was performed on the crystal structure of
human lysosomal α-glucosidase (PDB ID: 5NN5) and compared with acarbose as
a positive control. The activity of the PDZ-3Br-BZS compound was less good
activity in inhibiting the α-glucosidase enzyme, which is 2,481% and confirmed
by molecular docking studies that it only has one hydrogen bond interaction in
common with acarbose, that is with the amino acid Asp 616 and a large bond free
energy of -10 ,9567 kcal/mol compared to acarbose which is -18,2395 kcal/mol.
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