Synthesis and BZR affinity of pyrazolo[1,5-a]pyrimidine derivatives. Part 2: Further investigations on the 3-aryl substituents.

The synthesis and the in vitro affinities of a series of 3-aryl-4,7-dihydro -6-(N'-alkylpyrazol-3'- or 5'-yl)pyrazolo[1,5-a]pyrimidin-7-ones are descri bed in order to evaluate the conformational requirements of the lipophilic pockets into which the 3- and 6- substituents fit to provide better insight into the structure-affinity and activity relationship (SAFIR-SAR) of those compounds. The most promising compounds were tested in vivo.