Abstract
Naphthyridines, also known as diazanaphthalenes, are a group of heterocyclic compounds that include six isomeric bicyclic systems containing two pyridine rings. 1,6-Naphthyridines are one of the members of such a family capable of providing ligands for several receptors in the body. Among such structures, 1,6-naphthyridin-2(1H)-ones (7) are a subfamily that includes more than 17,000 compounds (with a single or double bond between C3 and C4) included in more than 1000 references (most of them patents). This review will cover the analysis of the diversity of the substituents present at positions N1, C3, C4, C5, C7, and C8 of 1,6-naphthyridin-2(1H)-ones, the synthetic methods used for their synthesis (both starting from a preformed pyridine or pyridone ring), and the biomedical applications of such compounds.
Highlights
The analysis of the substitution pattern at N1 of the 1,6-naphthyridin-2(1H)-ones with with a C5-C6 single bond (14) and with a C5-C6 double bond (13) (Table 1) shows that a C5-C6 single bond (14) and with a C5-C6 double bond (13)1 (Table 1) shows that comcompounds 14 have been usually left unsubstituted at N11 (R = H, 51.86% of structures pounds 14 have been usually left unsubstituted at N1 (R = H, 51.86% of structures dedescribed), while compounds 13 are usually substituted at such a position
In this case, such substitution patterns cover 63.06% of the total diversity. These results clearly show that the substitution pattern at C3 and C4 of the 1,6naphthyridin-2(1H)-ones with a C3-C4 single bond (14) is quite rich both in the level of substitution on each carbon atom and on the nature of the substituents present
We reviewed the substitution patterns of 1,6-naphthyridin-2(1H)-ones
Summary
Pharmaceuticals 2021, 14, At the beginning of any research project aimed at the development of new potential drug candidates for the treatment of a certain disease, one of the most important decisions to be taken is the selection of the central molecular structure (scaffold) on which to introduce the substituents needed to interact with the corresponding biological receptor. Such scaffolds can be selected based on the natural ligands of the receptor, the synthetic background of the research group, or, frequently, using the so-called privileged heterocyclic structures, a concept introduced by Evans in the late 1980s [1,2].
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