Identification of novel deoxyribofuranosyl indole antimicrobial agents

被引：35

作者：

Paudel, Atmika ^{[1
]}

Hamamoto, Hiroshi ^{[1
]}

Kobayashi, Yoshihisa ^{[2
]}

Yokoshima, Satoshi ^{[2
]}

Fukuyama, Tohru ^{[2
]}

Sekimizu, Kazuhisa ^{[1
]}

机构：

[1] Univ Tokyo, Microbiol Lab, Grad Sch Pharmaceut Sci, Tokyo, Japan

[2] Univ Tokyo, Lab Synthet Nat Prod Chem, Grad Sch Pharmaceut Sci, Tokyo, Japan

来源：

JOURNAL OF ANTIBIOTICS | 2012年 / 65卷 / 02期

关键词：

bactericidal; macromolecule synthesis; MRSA; novel antimicrobial; VRE; RESISTANT STAPHYLOCOCCUS-AUREUS; STEREOCONTROLLED TOTAL-SYNTHESIS; DAPTOMYCIN-RESISTANT; VANCOMYCIN; SUSCEPTIBILITY; BACTEREMIA; EMERGENCE; ISOLATE;

D O I：

10.1038/ja.2011.110

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Three novel deoxyribofuranosyl indole derivatives, FG050227 (1), FG050223 (2) and FG050204 (3), were identified as antimicrobial agents effective against Gram-positive bacterial strains and some fungi. The MIC values of (1), (2) and (3) against methicillin-resistant Staphylococcus aureus were 3.0, 6.0 and 13 mu gml(-1), respectively. Compounds 1 and 3 had bactericidal activity against exponentially growing S. aureus and inhibited biosynthesis of peptidoglycan, protein, RNA and DNA. Compound 2 was bacteriostatic and inhibited the biosynthesis of protein and RNA. The results indicated that deoxyribofuranosyl indole derivatives could be potential lead compounds for the development of antimicrobial agents. The Journal of Antibiotics (2012) 65, 53-57; doi: 10.1038/ja.2011.110; published online 14 December 2011

引用

页码：53 / 57

页数：5

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