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One-pot synthesis of new alkyl 1-naphthoates bearing quinoline, pyranone and cyclohexenone moieties metal-free sequential addition/oxidation reactions.一锅法合成含喹啉、吡喃酮和环己烯酮部分的新型烷基 1-萘甲酸酯——无金属顺序加成/氧化反应
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本文引用的文献

1
Drugs for bad bugs: confronting the challenges of antibacterial discovery.对抗耐药菌的药物:应对抗菌药物研发的挑战
Nat Rev Drug Discov. 2007 Jan;6(1):29-40. doi: 10.1038/nrd2201. Epub 2006 Dec 8.
2
Overview of nosocomial infections caused by gram-negative bacilli.革兰氏阴性杆菌引起的医院感染概述。
Clin Infect Dis. 2005 Sep 15;41(6):848-54. doi: 10.1086/432803. Epub 2005 Aug 16.
3
Clostridium difficile--associated diarrhea.艰难梭菌相关性腹泻
Am Fam Physician. 2005 Mar 1;71(5):921-8.
4
Severe community-onset pneumonia in healthy adults caused by methicillin-resistant Staphylococcus aureus carrying the Panton-Valentine leukocidin genes.携带杀白细胞素基因的耐甲氧西林金黄色葡萄球菌引起的健康成年人严重社区获得性肺炎。
Clin Infect Dis. 2005 Jan 1;40(1):100-7. doi: 10.1086/427148. Epub 2004 Dec 7.
5
Medicine. New TB drug promises shorter, simpler treatment.医学。新型结核病药物有望实现更短、更简便的治疗。
Science. 2004 Dec 10;306(5703):1872. doi: 10.1126/science.306.5703.1872.
6
Antibacterial resistance, Wayampis Amerindians, French Guyana.抗菌耐药性,瓦扬皮美洲印第安人,法属圭亚那
Emerg Infect Dis. 2004 Jun;10(6):1150-3. doi: 10.3201/eid1006.031015.
7
Ubiquinone and vitamin K in bacteria.细菌中的泛醌和维生素K。
Biochem J. 1962 Jun;83(3):606-14. doi: 10.1042/bj0830606.
8
Crystal structure of Mycobacterium tuberculosis MenB, a key enzyme in vitamin K2 biosynthesis.结核分枝杆菌MenB的晶体结构,维生素K2生物合成中的关键酶。
J Biol Chem. 2003 Oct 24;278(43):42352-60. doi: 10.1074/jbc.M307399200. Epub 2003 Aug 8.
9
SAM (dependent) I AM: the S-adenosylmethionine-dependent methyltransferase fold.SAM(依赖性)I AM:S-腺苷甲硫氨酸依赖性甲基转移酶折叠。
Curr Opin Struct Biol. 2002 Dec;12(6):783-93. doi: 10.1016/s0959-440x(02)00391-3.
10
Methicillin resistant Staphylococcus aureus (MRSA) in the intensive care unit.重症监护病房中的耐甲氧西林金黄色葡萄球菌(MRSA)
Postgrad Med J. 2002 Jul;78(921):385-92. doi: 10.1136/pmj.78.921.385.

1,4-二羟基-2-萘甲酸[校正后]异戊烯基转移酶抑制剂的发现:针对多重耐药革兰氏阳性病原体的新型药物先导物

Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.

作者信息

Kurosu Michio, Narayanasamy Prabagaran, Biswas Kallolmay, Dhiman Rakesh, Crick Dean C

机构信息

Department of Microbiology, Immunology, and Pathology, College of Veterinary Medicine and Biomedical Sciences, Colorado State University, 1682 Campus Delivery, Fort Collins, Colorado 80523-1682, USA.

出版信息

J Med Chem. 2007 Aug 23;50(17):3973-5. doi: 10.1021/jm070638m. Epub 2007 Jul 21.

DOI:10.1021/jm070638m
PMID:17658779
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2591091/
Abstract

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.

摘要

由于甲萘醌在电子传递系统中的利用是革兰氏阳性菌的一个特性,1,4 - 二羟基 - 2 - 萘甲酸异戊烯基转移酶(MenA)抑制剂1a和2a可作为针对耐甲氧西林金黄色葡萄球菌(MRSA)、表皮葡萄球菌(MRSE)和分枝杆菌属等细菌的选择性抗菌剂。耐药革兰氏阳性菌的生长对MenA抑制剂敏感,这表明甲萘醌合成是革兰氏阳性菌中一个有效的新药物靶点。