Senyawa Etil 4-{4-okso-2-[(E)-2-{4-sulfamoilfeniletenil}-3,4-dihidrokuinazolin-3-il]}benzoat merupakan senyawa baru yang mempunyai kemiripan strukturdengan senyawa diarilheterosiklik, sedangkan sebagian besar inhibitor selektifsiklooksigenase-2 merupakan senyawa diarilheterosiklik, sehingga senyawatersebut diprediksi mempunyai aktivitas menghambat konversi asam arakhidonatmenjadi prostaglandin melalui jalur siklooksigenase. Penelitian ini bertujuanuntuk menguji efek penghambatan siklooksigenase-2 (COX-2) oleh senyawa etil4-{4-okso-2-[(E)-2-{4-sulfamoilfeniletenil}-3,4-dihidrokuinazolin-3-il]}benzoat.Uji aktivitas penghambatan COX-2 dilakukan dengan menggunakan kit COX(ovine) inhibitor screening assay. Prostaglandin yang terbentuk ditentukanmenggunakan metoda Enzyme Immunoassay dan intensitas warna yang dihasilkandiukur serapannya menggunakan plate reader pada panjang gelombang 415 nm.Dari hasil uji didapatkan nilai IC50 senyawa etil 4-{4-okso-2-[(E)-2-{4-sulfamoilfeniletenil}-3,4-dihidrokuinazolin-3-il]}benzoat adalah 16,91 μM.Sebagai pembanding, pengujian juga dilakukan terhadap asetosal dan selekoksib.Hasil yang diperoleh untuk nilai IC50 asetosal dan selekoksib berturut-turut yaitu24,97 μM dan 0,43 μM. Hasil penelitian menunjukkan bahwa senyawa etil 4-{4-okso-2-[(E)-2-{4-sulfamoilfeniletenil}-3,4-dihidrokuinazolin-3-il]}benzoatmempunyai potensi inhibisi lebih kuat dibandingan asetosal tetapi masih lebihrendah dibandingkan selekoksib.
Abstract
Ethyl 4-{4-oxo-2-[(E)-2-{4-sulfamoylphenyletenyl}-3,4-dihydroquinazolin-3-yl]}benzoate compound is a new drug that has structural similarities with diarylheterocyclic compound, while some of cyclooxygenase-2 selective inhibitor is adiaryl heterocyclic compound, so that the compound is predicted to have activityinhibits the conversion of arachidonic acid into prostaglandins through thecyclooxygenase. The aim of this study is to the test inhibitory effect ofcyclooxygenase-2 (COX-2) by the ethyl 4-{4-oxo-2-[(E)-2-{4-sulfamoylphenyletenyl}-3,4-dihydroquinazolin-3-yl]}benzoate compound. Studyof COX-2 inhibitory activity carried out by using a kit COX (ovine) inhibitorscreening assay. Prostaglandins which were formed was determined using themethod of Enzyme Immunoassay and the resulting color intensity was measuredusing a plate reader absorbance at a wavelength of 415 nm. From the test resultsobtained IC50 value of ethyl 4-{4-oxo-2-[(E)-2-{4-sulfamoylphenyletenyl}-3,4-dihydroquinazolin-3-yl]}benzoate compound was 16.91 μM. For comparison, thetests were also done on acetosal and celecoxib. The results obtained for acetosaland celecoxib IC50 values were 24.97 μM and 0.43 μM, respectively. The resultsshowed that the ethyl 4-{4-oxo-2-[(E)-2-{4-sulfamoylphenyletenyl}-3,4-dihydroquinazolin-3-yl]}benzoate compound has stronger inhibitory potencycompared to acetosal but still lower than celecoxib. |
