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Derek Maclean

Publications and source records attributed to Derek Maclean.

4 recordsLinked to original sources
PubMed2003

Safety-catch linker strategies for the production of radiopharmaceuticals labeled with positron-emitting isotopes.

A novel synthetic stratetegy for compounds labeled with the positron-emitting isotope carbon-11 is described. The use of precursors attached to a solid support via safety-catch linkers allows selective release of radiolabeled material, leaving unreacted precursor attached to the support. Two different linkers demonstrate the application to the preparation of radiolabeled N-alkyl tertiary amines and N-alkylsulfonamides. This technique is expected to lead to more widespread use of positron emission tomography for the in vivo analysis of compound behavior.

Alkylation↗
PubMedDate not supplied

Drugs and probes: the symbiotic relationship between pharmaceutical discovery and imaging science.

Pharmaceutical research and imaging science are becoming increasingly intertwined. Positron emission tomography (PET) is a molecular imaging technique with particularly broad application in drug discovery and development. At the same time, modern techniques of drug discovery are helping accelerate the development of new PET probes. This article describes the relationship between the two fields, with particular consideration of practical and strategic limitations to full utilization of available technology.

Animals↗
PubMedDate not supplied

Agonists of the follicle stimulating hormone receptor from an encoded thiazolidinone library.

The design, synthesis, characterization, and screening of a large, encoded thiazolidinone library are described. Three sets of 35 building blocks were combined by encoded split-pool synthesis to give a library containing more than 42 000 members. Building block selection was based in part on a novel small molecule follicle stimulating hormone receptor agonist hit and in part for diversity. HPLC/MS techniques were applied at the single-bead level to build confidence in the reliability of library construction. Application of two distinct screening strategies resulted in the identification of compounds with significantly improved potency over the initial hit. This work demonstrates the versatility of encoded libraries for preparing a large number of analogues of a given hit while simultaneously generating a large collection of compounds for screening against other targets.

Aldehydes↗