Spiroacetals are attractive molecular frameworks for the development of high-quality compound collections for drug discovery projects. Firstly, these moieties play a key role in the biological outcome of the entire compound, whether directly interacting with the biological target or acting as a scaffold to address side chains into specific directions. Secondly, the distinct conformational flexibility of these frameworks assists the molecule in assuming the three-dimensional profile required for optimal binding to a biomacromolecule, resulting in a variety of different structural arrangements and subsequent biological outcomes. Modern advances in the efficient and selective synthesis of these skeletons are giving a great impulse in the use of acetal chemistry for the production of high-quality compound collections. In this chapter, we highlight the most versatile strategies to access spiroacetal molecular frameworks, and we report three examples of the synthesis of acetal-containing small molecule collections, together with the discussion of their biological outcomes.

Synthesis and biological properties of spiroacetal-containing small molecules / Lenci E.. - STAMPA. - (2020), pp. 225-245. [10.1016/B978-0-12-818349-6.00008-X]

Synthesis and biological properties of spiroacetal-containing small molecules

Lenci E.
2020

Abstract

Spiroacetals are attractive molecular frameworks for the development of high-quality compound collections for drug discovery projects. Firstly, these moieties play a key role in the biological outcome of the entire compound, whether directly interacting with the biological target or acting as a scaffold to address side chains into specific directions. Secondly, the distinct conformational flexibility of these frameworks assists the molecule in assuming the three-dimensional profile required for optimal binding to a biomacromolecule, resulting in a variety of different structural arrangements and subsequent biological outcomes. Modern advances in the efficient and selective synthesis of these skeletons are giving a great impulse in the use of acetal chemistry for the production of high-quality compound collections. In this chapter, we highlight the most versatile strategies to access spiroacetal molecular frameworks, and we report three examples of the synthesis of acetal-containing small molecule collections, together with the discussion of their biological outcomes.
9780128183496
Small Molecule Drug Discovery: Methods, Molecules and Applications
225
245
Lenci E.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2158/1281727
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