Parallel-compound synthesis: methodology for accelerating drug discovery.
Parallel compound synthesis enables large numbers of individual compounds to be prepared simultaneously using semiautomated techniques. This fast and efficient methodology has an important role to play in accelerating lead optimisation and hence the whole drug discovery process. The potential of this strategy to rapidly optimise chemical leads and provide structure-activity relationship (SAR) information was demonstrated in two therapeutic areas, antiviral agents (herpes simplex virus), and neurokinin-2 receptor antagonists.
Selway
C N
CN
Discovery Chemistry Department, Pfizer Central Research, Sandwich, Kent, UK.
Terrett
N K
NK
D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001667:Binding, Competitive; D016466:CHO Cells / Q000166:cytology / Q000378:metabolism; D002522:Chlorocebus aethiops; D006224:Cricetinae; D004265:DNA Helicases / Q000037:antagonists & inhibitors; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods* / Q000706:statistics & numerical data; D004345:Drug Industry / Q000379:methods; D018259:Herpesvirus 1, Human / Q000187:drug effects* / Q000201:enzymology / Q000254:growth & development; D009682:Magnetic Resonance Spectroscopy; D015288:Neurokinin A / Q000819:agonists / Q000138:chemical synthesis / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis*; D011869:Radioligand Assay; D051381:Rats; D018041:Receptors, Neurokinin-2 / Q000032:analysis / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014709:Vero Cells / Q000166:cytology; D010948:Viral Plaque Assay / Q000379:methods
D000998:Antiviral Agents; D004364:Pharmaceutical Preparations; D018041:Receptors, Neurokinin-2; D015288:Neurokinin A; D004265:DNA Helicases