-transparent.png){kind=logo}
Synthesis and biological evaluation of 8-aminomethyltetracycline derivatives as novel antibacterial agents. 2013
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
Discovery Chemistry, ‡Microbiology, and §Process Chemistry R&D, Tetraphase Pharmaceuticals, Inc. , 480 Arsenal Street, Watertown, Massachusetts 02472, United States.
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.
Related Publications
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
February 2009,
European journal of medicinal chemistry,
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
October 2013,
European journal of medicinal chemistry,
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
June 2023,
Bioorganic & medicinal chemistry letters,
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
April 2021,
Bioorganic chemistry,
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
July 2021,
ACS omega,
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
October 2012,
Bioorganic & medicinal chemistry letters,
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
July 2005,
Bioorganic & medicinal chemistry letters,
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
November 2014,
Molecules (Basel, Switzerland),
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
April 2014,
Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society,
Roger B Clark, and
Minsheng He, and
Yonghong Deng, and
Cuixiang Sun, and
Chi-Li Chen, and
Diana K Hunt, and
William J O'Brien, and
Corey Fyfe, and
Trudy H Grossman, and
Joyce A Sutcliffe, and
Catherine Achorn, and
Philip C Hogan, and
Christopher E Katz, and
John Niu, and
Wu-Yan Zhang, and
Zhijian Zhu, and
Magnus Ronn, and
Xiao-Yi Xiao
May 2024,
Bioorganic & medicinal chemistry letters,
