Heterocycle-Based Multicomponent Reactions in Drug Discovery: From Hit Finding to Rational Design

In the context of the structural complexity necessary for a molecule to selectively display a therapeutical action and the requirements for suitable pharmacokinetics, a robust synthetic approach is essential. Typically, thousands of relatively similar compounds should be prepared along the drug disc...

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Detalhes bibliográficos
Autores: Nadal Rodríguez, Pau, Ghashghaei, Ouldouz, Bagan Polonio, Andrea, Escolano Mirón, Carmen, Lavilla Grífols, Rodolfo
Formato: artículo
Estado:Versión publicada
Fecha de publicación:2022
País:España
Recursos:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/187141
Acesso em linha:https://hdl.handle.net/2445/187141
Access Level:acceso abierto
Palavra-chave:Química farmacèutica
Síntesi orgànica
Compostos heterocíclics
Pharmaceutical chemistry
Organic synthesis
Heterocyclic compounds
Descrição
Resumo:In the context of the structural complexity necessary for a molecule to selectively display a therapeutical action and the requirements for suitable pharmacokinetics, a robust synthetic approach is essential. Typically, thousands of relatively similar compounds should be prepared along the drug discovery process. In this respect, heterocycle‐based multicomponent reactions offer advantages over traditional stepwise sequences in terms of synthetic economy, as well as the fast access to chemsets to study the structure activity relationships, the fine tuning of properties, and the preparation of larger amounts for preclinical phases. In this account, we briefly summarize the scientific methodology backing the research line followed by the group. We comment on the main results, clustered according to the targets and, finally, in the conclusion section, we offer a general appraisal of the situation and some perspectives regarding future directions in academic and private research.