Design at the atomic level: Design of biaryloxazolidinones as potent orally active antibiotics

被引：47

作者：

Zhou, Jiacheng ^{[2
]}

Bhattacharjee, Ashoke ^{[2
]}

Chen, Shili ^{[2
]}

Chen, Yi ^{[2
]}

Duffy, Erin ^{[1
]}

Farmer, Jay ^{[2
]}

Goldberg, Joel ^{[2
]}

Hanselmann, Roger ^{[2
]}

Ippolito, Joseph A. ^{[1
]}

Lou, Rongliang ^{[2
]}

Orbin, Alia ^{[2
]}

Oyelere, Ayomi ^{[2
]}

Salvino, Joe ^{[2
]}

Springer, Dane ^{[2
]}

Tran, Jennifer ^{[2
]}

Wang, Deping ^{[1
]}

Wu, Yusheng ^{[2
]}

Johnson, Graham ^{[1
,2
]}

机构：

[1] Rib X Pharmaceut Inc, Dept Struct Based Drug Design, New Haven, CT 06511 USA

[2] Rib X Pharmaceut Inc, Dept Med Chem, New Haven, CT 06511 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 23期

关键词：

Oxazolidinone; Biaryloxazolidinone; Structure-based drug design; Linezolid; Sparsomycin; Gram-negative bacteria; X-ray crystal structure; Ribosome; Oral antibiotics; Hybrid antibiotics;

D O I：

10.1016/j.bmcl.2008.10.011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have developed a first generation of hybrid sparsomycin -linezolid compounds into a new family of orally bioavailable biaryloxazolidinones that have activity against both linezolid-susceptible and -resistant Gram-positive bacteria as well as the fastidious Gram-negative bacteria Haemophilus influenzae and Moraxella catarrahalis. The convergent synthesis of these new compounds is detailed. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6175 / 6178

页数：4

共 7 条

[1] Recent advances in oxazolidinone antibacterial agent research [J].

Hutchinson, DK .

EXPERT OPINION ON THERAPEUTIC PATENTS, 2004, 14 (09) :1309-1328

[2] Carbon-carbon-linked (pyrazolylphenyl)oxazolidinones with antibacterial activity against multiple drug resistant gram-positive and fastidious gram-negative bacteria [J].

Lee, CS ;

Allwine, DA ;

Barbachyn, MR ;

Grega, KC ;

Dolak, LA ;

Ford, CW ;

Jensen, RM ;

Seest, EP ;

Hamel, JC ;

Schaadt, RD ;

Stapert, D ;

Yagi, BH ;

Zurenko, GE ;

Genin, MJ .

BIOORGANIC & MEDICINAL CHEMISTRY, 2001, 9 (12) :3243-3253

[3]

*NCCLS, 2001, M7 A5 METHODS DILUTI

[4] Design at the atomic level: Generation of novel hybrid biaryloxazolidinones as promising new antibiotics [J].

Zhou, Jiacheng ;

Bhattacharjee, Ashoke ;

Chen, Shili ;

Chen, Yi ;

Duffy, Erin ;

Farmer, Jay ;

Goldberg, Joel ;

Hanselmann, Roger ;

Ippolito, Joseph A. ;

Lou, Rongliang ;

Orbin, Alia ;

Oyelere, Ayomi ;

Salvino, Joe ;

Springer, Dane ;

Tran, Jennifer ;

Wang, Deping ;

Wu, Yusheng ;

Johnson, Graham .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (23) :6179-6183

[5]

6689779

[6]

5254577

[7]

7192974

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