ChemInform Abstract: Synthetic Strategies in Combinatorial Chemistry

Spaller, Mark R.; Burger, Matthew T.; Fardis, Maria; Bartlett, P. A.

doi:10.1002/chin.199742340

Cited by 2 publications

(2 citation statements)

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“…A review article from 1997 by Spaller et al suggested that combinatorial libraries may be suggested to fall into two categories: focused libraries, where a number of closely related compounds based on a privileged structure are synthesized with a known target in mind, and prospecting libraries, where an entirely new lead compound is sought, so the objective is to screen a large number of structurally varied compounds in the hope of finding a lead with a novel mode of action [29]. The focused libraries can be considered to be the result of a "classical" combinatorial chemistry approach, and further reference made here to combinatorial chemistry refers to the synthesis of this type of library.…”

Section: Small Molecules and Biologymentioning

confidence: 99%

Yeast as a Model in High‐Throughput Screening of Small‐Molecule Libraries

Stefanini

Filippo

Cavalieri

2013

Diversity‐Oriented Synthesis

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THE BASICS OF DIVERSITY-ORIENTED SYNTHESIS targets and their small molecule regulators" [1]. For TOS compounds, knowledge of the preselected targets can lead to some degree of rational design being implemented; however, according to Schreiber, the second class of library should benefit from high levels of structural diversity within the compound collection, so the deliberate synthesis of such libraries can be considered to be DOS. An alternative definition was offered later by our group, where it was suggested that "diversity-oriented synthesis involves the deliberate, simultaneous and efficient synthesis of more than one target compound in a diversity-driven approach to answer a complex problem" [2]. This statement leaves some room for interpretation; however, as the very nature of diversity, in a chemical sense, is to some degree subjective, it provides a useful general definition that can be applied across the majority of the examples of DOS that are published today. The "complex problem" mentioned in this definition usually refers to the discovery of novel biologically relevant compounds, and this is the context in which DOS is usually discussed. However, as mentioned, this does not have to be the case, as the DOS approach could potentially be applied to other problems, such as the discovery of a novel ligand or catalyst for a reaction [2].

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Section: Small Molecules and Biologymentioning

confidence: 99%

Yeast as a Model in High‐Throughput Screening of Small‐Molecule Libraries

Stefanini

Filippo

Cavalieri

2013

Diversity‐Oriented Synthesis

View full text Add to dashboard Cite

show abstract

“…The increasing significance of combinatorial chemistry in pharmaceutical and material sciences is well recognized, which demands the development of new strategies to generate a collection of analogues of interesting compounds . It is well documented that imidazole or benzoimidazole derivatives are of particular interest for drug discovery since they are known to elicit a broad spectrum of biological activities, and their applications in diverse therapeutic areas (including antivirals, antitumor, antifungals, etc) have been discovered .…”

Section: Introductionmentioning

confidence: 99%