SAR for thioaryl linker modification

August 16, 2024

• Title:       

  SAR for thioaryl linker modification

• Image Source:

  Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors

• Mark:

  Table 2

• Associated context:

  A profound increase in biochemical potency was observed upon the introduction of substituents on the central thiophenyl ring (Table 2). A methyl group scan revealed the importance of such substitution at the  C4- or C6-position of the phenyl ring (9d–e). A wide variety of small substituents (9e–i) is tolerated at the C4-position.