title: Compound high-quality criteria: a new vision to guide the development of drugs, current situation.
abstract: For several decades, the pharmaceutical industry has suffered due to major issues such as reductions of the number of FDA approved drugs and biologics. Several analyses have been highlighted that the 'druglikeness' is one of the strategies to improve succeed rates of screening such as, for instance, high-throughput screening (HTS), and then hits (as starting point), leads and clinical candidates. It is clear that the improvement of compound quality accelerates the drug discovery projects. The monitoring of several indices to avoid 'molecular obesity' (ADMET problems) of final drugs from good-quality 'low-fat' starting points represents today a powerful strategy of optimization process. The development of the new guides to find drugs highlighting attempts at improving the attrition rate from hits to final medicines by focusing on how to improve the druggability of hits, leads and drugs during the drug discovery process represents a key approach to design next better generation of medicines.
authors.affiliation: Université Paris Descartes, PRES Sorbonne Paris Cité, CNRS UMR 860, Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologique, 45, rue des Saints Pères, 75006 Paris, France. Electronic address: serge.mignani@parisdescartes.fr.
authors.forename: Serge
authors.initials: S
authors.lastname: Mignani
authors.affiliation: SCYNEXIS, Inc., P.O. Box 12878, Research Triangle Park, NC 27709, USA.
authors.forename: Scot
authors.initials: S
authors.lastname: Huber
authors.affiliation: CQM - Centro de Química da Madeira, MMRG, Universidade da Madeira, Campus Universitário da Penteada, 9000-390 Funchal, Portugal.
authors.forename: Helena
authors.initials: H
authors.lastname: Tomás
authors.affiliation: CQM - Centro de Química da Madeira, MMRG, Universidade da Madeira, Campus Universitário da Penteada, 9000-390 Funchal, Portugal. Electronic address: joaor@uma.pt.
authors.forename: João
authors.initials: J
authors.lastname: Rodrigues
authors.affiliation: Laboratoire de Chimie de Coordination du CNRS, 205 route de Narbonne, BP 44099, 31077 Toulouse Cedex 4, France; Université de Toulouse, UPS, INPT, 31077 Toulouse Cedex 4, France. Electronic address: majoral@lcc-toulouse.fr.
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Majoral
mesh_terms: D055808:Drug Discovery; D004345:Drug Industry; D006801:Humans