首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Ester and hydroxamate analogues of methionyl and isoleucyl adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.
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Ester and hydroxamate analogues of methionyl and isoleucyl adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.

机译:甲硫酰基和异亮氨酰基腺苷酸的酯和异羟肟酸酯类似物作为甲硫酰基-tRNA和异亮氨酰-tRNA合成酶的抑制剂。

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摘要

The structure activity relationship on a series of ester and hydroxamate analogues of methionyl and isoleucyl adenylate has been investigated through introducing linkers between the 1'-position of ribose and adenine surrogates as methionyl-tRNA, and isoleucyl-tRNA synthetase inhibitors, respectively. The results indicate that ester analogue 23 was found to be a potent inhibitor of Escherichia coli methionyl-tRNA synthetase, and its interaction with the active site was proposed by a molecular modeling study.
机译:通过分别在核糖和腺嘌呤替代物的1'-位之间引入作为甲硫酰基-tRNA的异戊二酰基-tRNA合成酶抑制剂,研究了甲硫基和异亮氨酸-腺苷酸的一系列酯和异羟肟酸酯类似物的结构活性关系。结果表明,发现酯类似物23是大肠杆菌甲硫氨酸-tRNA合成酶的有效抑制剂,并且通过分子建模研究提出了其与活性位点的相互作用。

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