Advances in the Chemistry of Saccharins: From Synthetic Novelties Towards Biologically Active Compounds

Abstract

The saccharin ring system has gained considerable attention in the past decades, especially in the field of medicinal chemistry. The wide applicability of saccharin derivatives remains the driving force behind the constant development of novel routes and methods that provide new access to the construction of saccharin. Since the functionalization of this heterocycle has proved difficult, except for N- and O-alkylation, novel strategic approaches are much sought-after and thus constitute a great value to any medicinal chemist. In addition to the synthetic novelties introduced into the synthesis and functionalization of this particular heterocycle, the numerous newly discovered biological activities of saccharin and its derivatives are also reviewed. Saccharin may be considered to constitute a privileged framework on account of its role as a key structural element in several biologically active compounds ranging from enzyme inhibitors to receptor ligands and beyond.

Highly Active and Durable Nanocrystal‐Decorated Bifunctional Electrocatalyst for Rechargeable Zinc–Air Batteries

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Construction of Polycyclic γ-Lactams and Related Heterocycles via Electron Catalysis

“…1 Among them, the polycyclic γ-lactams have received considerable attention due to their important biological activities (Figure 1). For instance, salinosporamide A was isolated from a marine actinomycete by Fenical and co-workers, which has been proven to be a potent proteasome inhibitor.…”

Targeting COPD: advances on low‐molecular‐weight inhibitors of human neutrophil elastase

“…Saccharin is a heterocycle well known for its use as a sweetener but has gained considerable attention in the past decades in the field of medicinal chemistry due to its role as key structural element in several biologically active compounds . Saccharin‐like compounds were envisioned as mechanism‐based HNE inhibitors at the early 90's .…”