کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1408580 | 1501759 | 2014 | 6 صفحه PDF | دانلود رایگان |

• A series of 4-hydroxy-3-(naphthalen-1-ylmethyl)thiophen-2(5H)-ones were first synthesized.
• Compound 29 is the most potent agent against Staphylococcus aureus ATCC 25923 with MIC50 value of 0.21 μg/mL.
• Their biological activities are also evaluated for tyrosyl-tRNA synthase inhibitory activity.
A series of novel 4-hydroxy-3-(naphthalen-1-ylmethyl)thiophen-2(5H)-ones as tyrosyl-tRNA synthetase inhibitors were synthesized. Of these compounds, 4-(naphthalen-1-ylmethyl)-5-oxo-2,5-dihydrothiophen-3-yl-2-(4-hydroxyphenyl)acetate (29) was the most potent. The binding model and structure–activity relationship indicate that replacement of phenyl acetate in the side chain of 29 with a substituent containing more hydrophilic groups would be more suitable for further modification. Antibacterial assay revealed that the synthetic compounds are effective against growth of Gram-positive organisms, and 29 is the most potent agent against Staphylococcus aureus ATCC 25923 with MIC50 value of 0.21 μg/mL.
Journal: Journal of Molecular Structure - Volumes 1056–1057, 6 January 2014, Pages 104–109