The diversity‐oriented synthesis of pteridines—achievements and potential for development

Abstract

The importance of pteridines in the key cofactors, tetrahydrofolate and tetrahydrobiopterin, has encouraged the development of the chemistry and chemical biology of pteridines. In order to investigate the latter, versatile synthetic methods are required to prepare designed relatives of the natural cofactors for use as potential drugs or biological probes. Recently, diversity-oriented synthesis has become a particularly powerful and versatile approach to the synthesis of pteridines and related heterocyclic compounds. This article describes and discusses available methods using radical, electrophilic, nucleophilic, and organometal mediated substitution reactions.

Bicyclic 6-6 Systems: Pteridines

“…An excellent review article has been published on the methods available for diversification of the pteridine scaffold. 41…”

Therapeutic potential of pteridine derivatives: A comprehensive review

“…Nonetheless, other approaches are based on the linkage of a pteridine derivative to metal complexes or to molecules known to inhibit a specific target, with the objective of increasing their potency by targeting two different enzymes. Nevertheless, since chemical synthesis of pteridine derivatives is not the focus of this review, information about synthetic methods explaining how pteridine‐based compounds and drug candidates have been developed can be found in the comprehensive reviews by Suckling et al…”

Synthesis and Biological Evaluation of New Dipyridylpteridines, Lumazines, and Related Analogues

“…Pteridines, pyrazino[2,3‐ d ]pyrimidine compounds, are an important class of organic compounds for many biological processes, such as amino acid metabolism, nucleic acid synthesis, neurotransmitter synthesis, cancer, cardiovascular function, and growth and development of essentially all living organisms . The importance of pteridines in the key cofactors, tetrahydrofolate and tetrahydrobiopterin, has encouraged the development of the chemistry and chemical biology of pteridines . The pteridine nucleus is found to be essential component of various compounds possessing biological activities such as anti‐inflammatory , antimicrobial , anti‐hepatitis , immunosuppressive , antitumor , and neurodegenerative agents activities as well as α‐tumor nacrosis factor agents , adenosine kinase inhibitors , and nitric oxide synthase inhibitors .…”