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本文引用的文献

1
Active site directed inhibitors of replication-specific bacterial DNA polymerases.复制特异性细菌DNA聚合酶的活性位点定向抑制剂。
Bioorg Med Chem Lett. 2005 Feb 1;15(3):729-32. doi: 10.1016/j.bmcl.2004.11.016.
2
Synthesis of substituted 6-anilinouracils and their inhibition of DNA polymerase IIIC and Gram-positive bacterial growth.取代6-苯胺基尿嘧啶的合成及其对DNA聚合酶IIIC和革兰氏阳性菌生长的抑制作用。
J Med Chem. 2003 Jun 19;46(13):2731-9. doi: 10.1021/jm020591z.
3
DNA polymerases of low-GC gram-positive eubacteria: identification of the replication-specific enzyme encoded by dnaE.低GC含量革兰氏阳性真细菌的DNA聚合酶：由dnaE编码的复制特异性酶的鉴定
J Bacteriol. 2002 Jul;184(14):3834-8. doi: 10.1128/JB.184.14.3834-3838.2002.
4
Inhibitors of DNA polymerase III as novel antimicrobial agents against gram-positive eubacteria.DNA聚合酶III抑制剂作为抗革兰氏阳性真细菌的新型抗菌剂。
Antimicrob Agents Chemother. 1999 Aug;43(8):1982-7. doi: 10.1128/AAC.43.8.1982.
5
6-Anilinouracil-based inhibitors of Bacillus subtilis DNA polymerase III: antipolymerase and antimicrobial structure-activity relationships based on substitution at uracil N3.基于6-苯胺基尿嘧啶的枯草芽孢杆菌DNA聚合酶III抑制剂：基于尿嘧啶N3取代的抗聚合酶和抗菌构效关系
J Med Chem. 1999 Jun 3;42(11):2035-40. doi: 10.1021/jm980693i.
6
Compilation, alignment, and phylogenetic relationships of DNA polymerases.DNA聚合酶的汇编、比对及系统发育关系
Nucleic Acids Res. 1993 Feb 25;21(4):787-802. doi: 10.1093/nar/21.4.787.
7
Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives.非肽类血管紧张素II受体拮抗剂：一系列新型4,5-二氢-4-氧代-3H-咪唑并[4,5-c]吡啶衍生物的合成与生物活性
J Med Chem. 1994 May 27;37(11):1632-45. doi: 10.1021/jm00037a014.
8
Inhibitors of Bacillus subtilis DNA polymerase III. 6-Anilinouracils and 6-(alkylamino)uracils.枯草芽孢杆菌DNA聚合酶III的抑制剂。6-苯胺基尿嘧啶和6-（烷基氨基）尿嘧啶。
J Med Chem. 1980 Jan;23(1):34-8. doi: 10.1021/jm00175a007.
9
Inhibition of Bacillus subtilis deoxyribonucleic acid polymerase III by phenylhydrazinopyrimidines. Demonstration of a drug-induced deoxyribonucleic acid-enzyme complex.苯肼嘧啶对枯草芽孢杆菌脱氧核糖核酸聚合酶III的抑制作用。药物诱导的脱氧核糖核酸-酶复合物的证明。
J Biol Chem. 1975 Jan 25;250(2):522-6.
10
Synthesis and antiviral and enzymatic studies of certain 3-deazaguanines and their imidazolecarboxamide precursors.某些3-脱氮鸟嘌呤及其咪唑甲酰胺前体的合成、抗病毒和酶学研究。
J Med Chem. 1978 Dec;21(12):1212-8. doi: 10.1021/jm00210a008.

7-烷基-N(2)-取代的 3-去氮鸟嘌呤。合成、DNA 聚合酶 III 抑制和抗菌活性。

7-Alkyl-N(2)-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity.

机构信息

GLSynthesis Inc., One Innovation Drive, Worcester, MA 01605, USA.

出版信息

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4197-202. doi: 10.1016/j.bmcl.2011.05.093. Epub 2011 May 30.

DOI:10.1016/j.bmcl.2011.05.093
PMID:21684746
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3128661/
Abstract

Several 2-anilino- and 2-benzylamino-3-deaza-6-oxopurines [3-deazaguanines] and selected 8-methyl and 8-aza analogs have been synthesized. 7-Substituted N(2)-(3-ethyl-4-methylphenyl)-3-deazaguanines were potent and selective inhibitors of Gram+ bacterial DNA polymerase (pol) IIIC, and 7-substituted N(2)-(3,4-dichlorobenzyl)-3-deazaguanines were potent inhibitors of both pol IIIC and pol IIIE from Gram+ bacteria, but weakly inhibited pol IIIE from Gram- bacteria. Potent enzyme inhibitors in both classes inhibited the growth of Gram+ bacteria (MICs 2.5-10μg/ml), and were inactive against the Gram- organism Escherichia coli. Several derivatives had moderate protective activity in Staphylococcus aureus-infected mice.

摘要

已经合成了几种 2-苯胺基和 2-苯甲氨基-3-去氮-6-氧嘌呤[3-去氮鸟嘌呤]，并选择了一些 8-甲基和 8-氮杂类似物。7-取代的 N(2)-(3-乙基-4-甲基苯基)-3-去氮鸟嘌呤是革兰氏阳性菌 DNA 聚合酶（pol）IIIC 的有效且选择性抑制剂，而 7-取代的 N(2)-(3,4-二氯苄基)-3-去氮鸟嘌呤是革兰氏阳性菌的 pol IIIC 和 pol IIIE 的有效抑制剂，但对革兰氏阴性菌的 pol IIIE 抑制作用较弱。这两类强效酶抑制剂均能抑制革兰氏阳性菌的生长（MIC 为 2.5-10μg/ml），对革兰氏阴性菌大肠杆菌无活性。一些衍生物在金黄色葡萄球菌感染的小鼠中具有中等的保护活性。