8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents

被引：35

作者：

Clark, Roger B. ^{[1
]}

He, Minsheng ^{[1
]}

Fyfe, Corey ^{[1
]}

Lofland, Denene ^{[1
]}

O'Brien, William J. ^{[1
]}

Plamondon, Louis ^{[1
]}

Sutcliffe, Joyce A. ^{[1
]}

Xiao, Xiao-Yi ^{[1
]}

机构：

[1] Tetraphase Pharmaceut Inc, Watertown, MA 02472 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 54卷 / 05期

关键词：

PALLADIUM-CATALYZED AMINATION; CROSS-COUPLING REACTIONS; RESISTANCE DETERMINANTS; BACTERIAL-RESISTANCE; RIBOSOMAL-SUBUNIT; C-N; ANTIBIOTICS; 6-DEOXYTETRACYCLINES; EFFLUX; ROUTE;

D O I：

10.1021/jm1015389

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of fully synthetic 8-azatetracyclines was prepared and evaluated for antibacterial activity. Compounds were identified that overcome both efflux (tet(K)) and ribosomal protection (tet(M)) tetracycline resistance mechanisms and are active against Gram-positive and Gram-negative organisms. Two compounds were identified that exhibit comparable efficacy to marketed tetracyclines in in vivo models of bacterial infection.

引用

页码：1511 / 1528

页数：18

共 42 条

[1]

[Anonymous], KIRKOTHMER ENCY CHEM

[2]

[Anonymous], M07A8 CLIN LAB STAND

[3] TETRACYCLINE [J].