Add time:08/26/2019         Source:sciencedirect.com

We have applied a fast and high-yielding method for the parallel amidation of 4-[4-(2-methoxyphenyl)piperazin-1-yl]-butylamine yielding analogs of the partial dopamine receptor agonist BP 897. Using this amino scaffold prepared in solution and polymer-bound carboxylic acid equivalents, we have synthesized a series of high affinity dopamine D3 receptor ligands. The novel compounds were obtained in good to excellent yield and purity. Biological evaluation included determination of binding affinities at hD2S and hD3 receptor subtypes. From the 22 novel structures presented here, compound 4v showed high affinity (Ki (hD3) 1.6 nM) and a 136-fold preference for the D3 receptor versus that for the D2 receptor subtype. Our results suggest that this derivatization technique is a useful method to speed up structure–activity relationships studies on dopamine receptor subtype modulators.

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