title: Chemistry strategies in early drug discovery: an overview of recent trends.
abstract: In the scenario of a continuous request for better drugs in shorter times, medicinal chemists must face the challenging task of preparing new patentable molecules, combining high activity and selectivity, drug-likeness and good pharmacokinetic properties. Multiparametric optimization requires a substantial improvement of the efficacy and throughput of the early discovery process, leading to a significant revolution in organic synthesis and chemistry technologies. Chemists are searching for ways to simplify synthetic protocols, for example, by the use of polymer-assisted solution-phase synthesis, microwave-assisted organic synthesis and flow chemistry. Organic synthesis is benefiting of fast and robust reactions, with breakthrough approaches often entailing the privileged use of multicomponent reactions, click chemistry and ring-closing metathesis.
authors.affiliation: NiKem Research srl, via Zambeletti 25, 20021 Baranzate (Milan), Italy. matteo.colombo@nikemresearch.com
authors.forename: Matteo
authors.initials: M
authors.lastname: Colombo
authors.forename: Ilaria
authors.initials: I
authors.lastname: Peretto
mesh_terms: D055808:Drug Discovery / Q000639:trends*; D004341:Drug Evaluation; D004345:Drug Industry / Q000639:trends*; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis*; D012106:Research / Q000639:trends; D013678:Technology, Pharmaceutical / Q000639:trends
chemical_list: D004364:Pharmaceutical Preparations