Combinatorial Chemistry and the Synthesis of Compound Libraries

Author(s):  
Rolf Breinbauer ◽  
Matthias Mentel
2021 ◽  
Author(s):  
Claudine Herlan ◽  
Dominik Feser ◽  
Ute Schepers ◽  
Stefan Bräse

Combinatorial chemistry allows for the rapid synthesis of large compound libraries for high throughput screenings in biology, medicinal chemistry, or materials science. Especially compounds from a highly modular design are...


ChemInform ◽  
2010 ◽  
Vol 41 (52) ◽  
pp. no-no
Author(s):  
Rolf Breinbauer ◽  
Matthias Mentel

1998 ◽  
Vol 3 (1) ◽  
pp. 55-62 ◽  
Author(s):  
Kevin R. Oldenburg ◽  
Ji-Hu Zhang ◽  
Tongming Chen ◽  
Anthony Maffia ◽  
Karl F. Blom ◽  
...  

Combinatorial chemistry has opened a new realm of chemical entities in the search for novel therapeutics. Combinatorial chemistry is currently adding hundreds of thousands of compounds to similar numbers available from years of synthesis by medicinal chemistry. It is not unreasonable to expect that over the next several years, nearly a million compounds will be available for screening against each therapeutic target. The number of potential targets will also be increasing with the advances in genomics. With the increasing number of compounds to be screened against an increasing number of targets, it is becoming increasingly difficult and costly to obtain the required amounts of key biological material needed to screen these compounds. One obvious solution is to miniaturize the assays so that the biological reagent supply doesn't need to increase. To this end, we have developed an ultra-high throughput screening system comprised of a new plate design (9600-well), detection system, and liquid handling system. This new format is capable of performing assays in as little as 0.2 Al. The results obtained from this system compare favorably to those obtained in the standard 96-well format.


1994 ◽  
Vol 116 (6) ◽  
pp. 2661-2662 ◽  
Author(s):  
Chixu Chen ◽  
Lisa A. Ahlberg Randall ◽  
R. Bryan Miller ◽  
A. Daniel Jones ◽  
Mark J. Kurth

2003 ◽  
Vol 804 ◽  
Author(s):  
Peter Geissinger ◽  
Barry J. Prince ◽  
Nadejda T. Kaltcheva ◽  
Maureen J. Prince ◽  
Alan W. Schwabacher

ABSTRACTOur recently introduced “Fiber-Optic Combinatorial Chemistry” technique combines combinatorial synthetic methods and optical fiber sensor technologies. Our one-dimensional combinatorial chemistry method allows for synthesis of large compound libraries in a linear format, for example in the cladding of optical fibers. Subjecting these libraries to assays that indicate positive identification of a library member by the binding of a fluorescent group, produces, in effect, an optical fiber sensor array. The location of a particular fluorescent region along the optical fiber can be determined through the optical time-of-flight technique, in which laser pulses propagating through the fiber core probe through their evanescent fields the fluorescent properties of the compounds located in the fiber cladding. It is a virtue of our combinatorial synthetic procedure that with the location of a compound on the fiber, its synthetic history is immediately known. We demonstrated that limitations on the spatial resolution of compounds along the fiber due to the excited state lifetimes of the fluorescent marker molecules can be overcome by the use of a second fiber - evanescently coupled to the first one - as an optical delay.The existing claddings of optical fibers severely restrict the range of chemistries for the synthesis of combinatorial libraries. Therefore, in order to make our method more generally applicable, the existing fiber cladding has to be replaced by a porous material that can act as solid support for reactions and at the same time preserve the optical guiding conditions of the fiber. In this contribution we discuss the requirements for such a replacement cladding and evaluate the general suitability of a functionalized candidate material.


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