Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA.
J Nat Prod. 2009 Mar 27;72(3):496-9. doi: 10.1021/np800664u.
The effectiveness of precursor-directed biosynthesis to generate diazepinomicin (1) analogues with varied ring-A substitutents was investigated by feeding commercially available, potential ring-A precursors such as fluorinated tryptophans, halogenated anthranilates, and various substituted indoles into growing actinomycete culture DPJ15 (genus Micromonospora). Two new monofluorinated diazepinomicin analogues (2 and 3) were identified and characterized by spectroscopic methods. Both derivatives showed modest antibacterial activity against the Gram-positive coccus Staphylococcus aureus with MIC values in the range 8-32 microg/mL.
通过向生长中的放线菌 DPJ15（属 Micromonospora）培养物中添加市售的潜在环 A 前体，如氟化色氨酸、卤代邻氨基苯甲酸酯和各种取代吲哚，研究了前体定向生物合成生成具有不同环 A 取代基的二氮杂环庚烷霉素 (1) 类似物的效果。通过光谱方法鉴定并表征了两种新的单氟化二氮杂环庚烷霉素类似物 (2 和 3)。两种衍生物对革兰氏阳性球菌金黄色葡萄球菌均显示出适度的抗菌活性，MIC 值在 8-32μg/mL 范围内。
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