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Synthetic diversity-oriented synthesis

Contributions by R. Joseph and P. Arya as well as M. A. Koch and H. Waldmann focus on synthetic aspects towards lead structures originating from natural product-derived scaffolds. R. Joseph and P. Arya refer to two complementary approaches, the synthetic access to focussed libraries around bioactive natural product cores, and diversity-oriented synthesis aiming at 3D scaffold diversity for hit generation, respectively. On the other hand, M. A. Koch and H. Waldmann emphasise the correlation of natural product-based library concepts with structural features of targeted protein domains, thus strengthening the privileged structure concept from a bioorganic viewpoint. [Pg.483]

Diversity-oriented synthesis of small molecules is a great challenge for synthetic organic chemists. DOS requires the development of new methodologies that generate scaffold diversity in addition to appendage and stereochemical diversity. [Pg.123]

Most commonly, a commercial library, containing a subset of compounds that matches a desired set of properties (if known), is screened in an initial study. Once hits are obtained and verified, a small library of compounds is synthesized to produce a set of compounds in the same chemical-stmctural space as the original hit stmcture. This process allows for hits with higher potency and elucidates information of the structure-activity relationship within the system of interest. Such synthetic libraries of chemically diverse compounds have been made possible through combinatorial chemistry (52-56) and diversity-oriented synthesis (52). [Pg.2215]

Spring, D. R. Diversity-oriented synthesis a challenge for synthetic chemists. Org. Biomol. Chem. 2003,1, 3867—3870. [Pg.206]

Figure 6.28 Some different scaffolds prepared through diversity oriented synthesis (DOS). (Taylor, S. J. et al. Synthetic strategy toward skeletal diversity via solid-supported, otherwise unstable reactive intermediates. Angew. Chem. Int. Ed. Engl. 2004, 43, 1681-1685.) ... Figure 6.28 Some different scaffolds prepared through diversity oriented synthesis (DOS). (Taylor, S. J. et al. Synthetic strategy toward skeletal diversity via solid-supported, otherwise unstable reactive intermediates. Angew. Chem. Int. Ed. Engl. 2004, 43, 1681-1685.) ...
Towards drugging the undrug-gable enhancing the scaffold diversity of synthetic small molecule screening collections using diversity-oriented synthesis. Divers. Oriented Synth., 1, 21-28. [Pg.389]

Diversity-oriented synthesis (DOS) was defined by Schreiber in 2000 [34]. He referred to synthetic processes that contain only a few steps ( 3-5) and are planned with a forward... [Pg.7]


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See also in sourсe #XX -- [ Pg.108 , Pg.109 ]




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