2-Hydroxy-N′-(4-fluorobenzoyl)benzohydrazide

Santosa, Harry; Yuniarta, Tegar Achsendo; Kesuma, Dini; Putra, Galih Satrio

doi:10.3390/m1103

Cited by 4 publications

(1 citation statement)

References 22 publications

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“…Accordingly, C-F carbon splitting (160 and 163 ppm, J: 245 Hz) is consistent with the literature data. C-H carbon splittings in the neighborhood of fluorine (115.8 and 116.02, J: 21.6 Hz) also met the literature and expected data [ 21 ].…”

Section: Discussionsupporting

confidence: 82%

Synthesis, characterization, COX1/2 inhibition and molecular modeling studies on novel 2-thio-diarylimidazoles

2021

Turk J Chem

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Heterocyclic compounds with diaryl substituents have been a milestone approach for selective cyclooxygenase 2 (COX 2) inhibition by bioisosteric replacements and modifications. It is also known that thiazole derivatives have different pharmacological activities. In this study, nine novel 2-[(1,5-diphenyl-1H-imidazole-2-yl)thio]-N-(thiazole-2-yl)acetamide derivatives (Compound 1-9) were synthesized via the reaction of 1,5-disubstitued phenyl-imidazole-2-thiole and N-thiazole acetamide. The inhibitory effects of COX-1 and COX-2 enzymes were tested for the synthesized compounds.Enzyme-ligand interactions of the most active compound on COX subtypes were elucidated by molecular modelling studies. The percent inhibitory effect for compound 1, which is the naked derivative among all the compounds, was found to be the most active on COX-2 at 10 μM concentration (C1COX-2: 88%, SC-560COX-2: 98.2%, C1COX-1: 60.9%); whereas compound 9 showed the highest inhibitory effect and was found to be the most selective derivative on COX-1 isoenzyme (C9COX-1: 85%, DuP-697COX-1: 97.2%, C9COX-2: 57.9%)

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Section: Discussionsupporting

confidence: 82%