Chemistry strategies in early drug discovery: an overview of recent trends

Drug Discov Today. 2008 Aug;13(15-16):677-84. doi: 10.1016/j.drudis.2008.03.007. Epub 2008 May 2.

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.

Publication types

  • Review

MeSH terms

  • Drug Discovery / trends*
  • Drug Evaluation
  • Drug Industry / trends*
  • Pharmaceutical Preparations / chemical synthesis*
  • Research / trends
  • Technology, Pharmaceutical / trends

Substances

  • Pharmaceutical Preparations