Lead-Oriented Synthesis: A New Opportunity for Synthetic Chemistry
| Autor: | Alan Nadin, Ian Churcher, Channa K. Hattotuwagama |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
Molecular Structure
Combinatorial Chemistry Techniques Drug discovery business.industry Chemistry Chemistry Pharmaceutical media_common.quotation_subject Drug Evaluation Preclinical Compound management General Chemistry Combinatorial chemistry Catalysis Lead (geology) Pharmaceutical Preparations Drug development Drug Design Humans Quality (business) Biochemical engineering business Pharmaceutical industry media_common |
| Zdroj: | Angewandte Chemie International Edition. 51:1114-1122 |
| ISSN: | 1433-7851 |
| DOI: | 10.1002/anie.201105840 |
| Popis: | The pharmaceutical industry remains solely reliant on synthetic chemistry methodology to prepare compounds for small-molecule drug discovery programmes. The importance of the physicochemical properties of these molecules in determining their success in drug development is now well understood but we present here data suggesting that much synthetic methodology is unintentionally predisposed to producing molecules with poorer drug-like properties. This bias may have ramifications to the early hit- and lead-finding phases of the drug discovery process when larger numbers of compounds from array techniques are prepared. To address this issue we describe for the first time the concept of lead-oriented synthesis and the opportunity for its adoption to increase the range and quality of molecules used to develop new medicines. |
| Databáze: | OpenAIRE |
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