-transparent.png){kind=logo}
Design and synthesis of monocyclic beta-lactams as mechanism-based inhibitors of human cytomegalovirus protease. 1998
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
Department of Enzyme Medicinal Chemistry II, Glaxo Wellcome Research and Development, Medicines Research Centre, Stevenage, Herts, UK. adb3028@ggr.co.uk
Mechanism based inhibitors of HCMV protease have been designed based on the monocyclic beta-lactam nucleus, which have been shown to acylate the viral enzyme in a time dependent manner. SAR in a series of monocyclic beta-lactam N-ureas, has defined the size and relative stereochemistry of the C-3 substituent producing a low micromolar inhibitor 17b with good aqueous stability and selectivity over the mammalian serine proteases.
Related Publications
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
June 1998,
Bioorganic & medicinal chemistry letters,
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
February 2002,
Bioorganic & medicinal chemistry letters,
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
August 1993,
Biochemistry,
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
April 2011,
ACS chemical biology,
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
January 2004,
Molecules (Basel, Switzerland),
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
July 1998,
Journal of medicinal chemistry,
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
June 1975,
Journal of medicinal chemistry,
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
January 2006,
Molecules (Basel, Switzerland),
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
October 2000,
Bioorganic & medicinal chemistry letters,
A D Borthwick, and
G Weingarten, and
T M Haley, and
M Tomaszewski, and
W Wang, and
Z Hu, and
J Bedard, and
H Jin, and
L Yuen, and
T S Mansour
January 1984,
Scandinavian journal of infectious diseases. Supplementum,
