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- W3135649320 endingPage "2315" @default.
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- W3135649320 abstract "Privileged structures have been widely used as effective templates for drug discovery. While benzo-1,4-diazepine constitutes the first historical example of such a structure, the 1,3 analogue is just as rich in terms of applications in medicinal chemistry. The 1,3-diazepine moiety is present in numerous biological active compounds including natural products, and is used to design compounds displaying a large range of biological activities. It is present in the clinically used anticancer compound pentostatin, in several recent FDA approved β-lactamase inhibitors (e.g., avibactam) and also in coformycin, a natural product known as a ring-expanded purine analogue displaying antiviral and anticancer activities. Several other 1,3-diazepine containing compounds have entered into clinical trials. This heterocyclic structure has been and is still widely used in medicinal chemistry to design enzyme inhibitors, GPCR ligands, and so forth. This review endeavours to highlight the main use of the 1,3-diazepine scaffold and its derivatives, and their applications in medicinal chemistry, drug design, and therapy. We will focus more particularly on the development of enzyme inhibitors incorporating this scaffold, with a strong emphasis on the molecular interactions involved in the inhibition mechanism." @default.
- W3135649320 created "2021-03-15" @default.
- W3135649320 creator A5048887471 @default.
- W3135649320 creator A5052978566 @default.
- W3135649320 creator A5059303271 @default.
- W3135649320 date "2021-03-01" @default.
- W3135649320 modified "2023-10-18" @default.
- W3135649320 title "1,3‐Diazepine: A privileged scaffold in medicinal chemistry" @default.
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