Discovery of 1,4-dihydroxy-2-naphthoate prenyltransferase inhibitors: New drug leads for multidrug-resistant gram-positive pathogens
Discovery of 1,4-dihydroxy-2-naphthoate prenyltransferase inhibitors: New drug leads for multidrug-resistant gram-positive pathogens
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DOI：
10.1021/jm070638m
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发表时间：
2007-08-23
影响因子：
7.3
通讯作者：
Crick, Dean C.
中科院分区：
文献类型：
--
作者：
Kurosu, Michio;Narayanasamy, Prabagaran;Crick, Dean C.
由于甲基萘醌在电子传递系统中的利用是革兰氏阳性生物体的特征，因此1，4-二羟基-2-萘甲酸异戊烯基转移酶（MenA）抑制剂1a和2a作为选择性抗菌剂对抗生物体，例如耐甲氧西林金黄色葡萄球菌（MRSA）、表皮葡萄球菌（MRSE）和分枝杆菌属（Mycobacterium spp.）。耐药革兰氏阳性菌的生长对MenA抑制剂敏感，表明甲基萘醌合成是革兰氏阳性菌中有效的新药物靶标。
Since utilization of menaquinone in the electron transport system is a characteristic of Gram-positive organisms, the 1,4-dihydroxy-2-naphthoate prenyltransferase (MenA) inhibitors 1a and 2a act as selective antibacterial agents against organisms such as methicillin-resistant Stapylococcus aureus (MRSA), Staphylococcus epidermidis (MRSE), and Mycobacterium spp. Growth of drug-resistant Gram-positive organisms was sensitive to the MenA inhibitors, indicating that menaquinone synthesis is a valid new drug target in Gram-positive organisms.