Combinatorial Chemistry in the Drug Discovery Process

2006 ◽  
pp. 129-167 ◽  
Author(s):  
Ian Hughes
Keyword(s):  
Drug Discovery ◽  
Combinatorial Chemistry ◽  
Discovery Process ◽  
Drug Discovery Process

Combinatorial Chemistry in the Drug Discovery Process

1997 ◽  
Vol 14 (3-4) ◽  
pp. 231-241 ◽  
Author(s):  
Emile M. Bellott ◽  
Robert Bondaryk ◽  
Ann L. Luther
Keyword(s):  
Drug Discovery ◽  
Combinatorial Chemistry ◽  
Discovery Process ◽  
Drug Discovery Process

Combinatorial Chemistry in the Drug Discovery Process

2005 ◽  
pp. 961-1011
Author(s):  
Nathan T. Ross ◽  
Brian R. McNaughton ◽  
Benjamin L. Miller
Keyword(s):  
Drug Discovery ◽  
Combinatorial Chemistry ◽  
Discovery Process ◽  
Drug Discovery Process

scholarly journals Managing laboratory automation: integration and informatics in drug discovery

2000 ◽  
Vol 22 (6) ◽  
pp. 169-170 ◽  
Author(s):  
Charles J. Manly
Keyword(s):  
Drug Discovery ◽  
High Throughput ◽  
Combinatorial Chemistry ◽  
High Throughput Screening ◽  
Laboratory Automation ◽  
Discovery Process ◽  
Drug Discovery Process ◽  
Modern Drug

Drug discovery today requires the focused use of laboratory automation and other resources in combinatorial chemistry and high-throughput screening (HTS). The ultimate value of both combinatorial chemistry and HTS technologies and the lasting impact they will have on the drug discovery process is a chapter that remains to be written. Central to their success and impact is how well they are integrated with each other and with the rest of the drug discovery processes-informatics is key to this success. This presentation focuses on informatics and the integration of the disciplines of combinatorial chemistry and HTS in modern drug discovery. Examples from experiences at Neurogen from the last five years are described.

scholarly journals Hit-Optimization Using Target-Directed Dynamic Combinatorial Chemistry: Development of Inhibitors of the Anti-Infective Target 1-Deoxy-D-Xylulose-5-Phosphate Synthase

2020 ◽  
Author(s):  
Ravindra P. Jumde ◽  
Melissa Guardigni ◽  
Robin M. Gierse ◽  
Alaa Alhayek ◽  
Di Zhu ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Combinatorial Chemistry ◽  
Discovery Process ◽  
Drug Discovery Process ◽  
Biological Targets ◽  
Dynamic Combinatorial Chemistry ◽  
Structure Activity ◽  
Chemistry Development ◽  
Relationship Of ◽  
Phosphate Synthase

<p>Target-directed dynamic combinatorial chemistry (tdDCC) enables the identification, as well as optimization of ligands for un(der)explored targets such as the anti-infective target 1‑deoxy‑d‑xylulose-5-phosphate synthase (DXS). We report the unprecedented use of tdDCC to first identify and subsequently optimize inhibitors of the anti-infective target DXS. Using tdDCC, we were able to generate acylhydrazone-based inhibitors for DXS. The tailored tdDCC runs also provided insights into the structure–activity relationship of this novel class of DXS inhibitors. This approach holds the potential to expedite the drug discovery process and could be generally applied to a range of biological targets.</p>

scholarly journals Hit-Optimization Using Target-Directed Dynamic Combinatorial Chemistry: Development of Inhibitors of the Anti-Infective Target 1-Deoxy-D-Xylulose-5-Phosphate Synthase

2020 ◽  
Author(s):  
Ravindra P. Jumde ◽  
Melissa Guardigni ◽  
Robin M. Gierse ◽  
Alaa Alhayek ◽  
Di Zhu ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Combinatorial Chemistry ◽  
Discovery Process ◽  
Drug Discovery Process ◽  
Biological Targets ◽  
Dynamic Combinatorial Chemistry ◽  
Structure Activity ◽  
Chemistry Development ◽  
Relationship Of ◽  
Phosphate Synthase

<p>Target-directed dynamic combinatorial chemistry (tdDCC) enables the identification, as well as optimization of ligands for un(der)explored targets such as the anti-infective target 1‑deoxy‑d‑xylulose-5-phosphate synthase (DXS). We report the unprecedented use of tdDCC to first identify and subsequently optimize inhibitors of the anti-infective target DXS. Using tdDCC, we were able to generate acylhydrazone-based inhibitors for DXS. The tailored tdDCC runs also provided insights into the structure–activity relationship of this novel class of DXS inhibitors. This approach holds the potential to expedite the drug discovery process and could be generally applied to a range of biological targets.</p>

ReAction!

2009 ◽  
Author(s):  
Mark A. Griep ◽  
Marjorie L. Mikasen
Keyword(s):  
Drug Discovery ◽  
Chemical Weapons ◽  
Trial And Error ◽  
Discovery Process ◽  
Drug Discovery Process ◽  
Special Effects ◽  
Invisible Man ◽  
Feature Films ◽  
The World ◽  
Chemical Companies

ReAction! gives a scientist's and artist's response to the dark and bright sides of chemistry found in 140 films, most of them contemporary Hollywood feature films but also a few documentaries, shorts, silents, and international films. Even though there are some examples of screen chemistry between the actors and of behind-the-scenes special effects, this book is really about the chemistry when it is part of the narrative. It is about the dualities of Dr. Jekyll vs. inventor chemists, the invisible man vs. forensic chemists, chemical weapons vs. classroom chemistry, chemical companies that knowingly pollute the environment vs. altruistic research chemists trying to make the world a better place to live, and, finally, about people who choose to experiment with mind-altering drugs vs. the drug discovery process. Little did Jekyll know when he brought the Hyde formula to his lips that his personality split would provide the central metaphor that would come to describe chemistry in the movies. This book explores the two movie faces of this supposedly neutral science. Watching films with chemical eyes, Dr. Jekyll is recast as a chemist engaged in psychopharmaceutical research but who becomes addicted to his own formula. He is balanced by the often wacky inventor chemists who make their discoveries by trial-and-error.

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