1181458-21-8Relevant articles and documents
Synthesis and biological evaluation of 8-aminomethyltetracycline derivatives as novel antibacterial agents
Clark, Roger B.,He, Minsheng,Deng, Yonghong,Sun, Cuixiang,Chen, Chi-Li,Hunt, Diana K.,O'Brien, William J.,Fyfe, Corey,Grossman, Trudy H.,Sutcliffe, Joyce A.,Achorn, Catherine,Hogan, Philip C.,Katz, Christopher E.,Niu, John,Zhang, Wu-Yan,Zhu, Zhijian,Ronn, Magnus,Xiao, Xiao-Yi
, p. 8112 - 8138 (2013)
The C-8 position of the tetracyclines has been largely underexplored because of limitations in traditional semisynthetic techniques. Employing a total synthetic approach allowed for modifications at the C-7 and C-8 positions, enabling the generation of structure-activity relationships for overcoming the two most common tetracycline bacterial-resistance mechanisms: ribosomal protection (tet(M)) and efflux (tet(A)). Ultimately, several compounds were identified with balanced activity against both Gram-positive and Gram-negative bacteria, including pathogens bearing both types of tetracycline-resistance mechanisms. Compounds were screened in a murine systemic infection model to rapidly identify compounds with oral bioavailability, leading to the discovery of several compounds that exhibited efficacy when administered orally in murine pyelonephritis and pneumonia models.
Tetracycline compounds
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Page/Page column 181; 182; 183, (2016/05/19)
The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
SUBSTITUTED 4-AMINOBENZAMIDES AS KCNQ2/3 MODULATORS
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Page/Page column 135, (2013/11/05)
The invention relates to substituted 4-aminobenzamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
SUBSTITUTED 4-AMINOBENZAMIDES AS KCNQ2/3 MODULATORS
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Paragraph 0674, (2013/11/05)
Substituted 4-aminobenzamides, pharmaceutical compositions containing these compounds and also methods of using these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
TETRACYCLINE ANALOGS
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Page/Page column 62, (2012/03/09)
The present invention is directed to a compound represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.
POLYCYCLIC TETRACYCLINE COMPOUNDS
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Page/Page column 74-75, (2011/10/13)
The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.