Novel furan-2-carboxylic acid {ω-[4-(substituted phenyl)- piperazine-1-yl]alkyl} amide and 2-oxo-2H-chromene-3-carboxylic acid {ω -[4-(substituted phenyl)-piperazine-1-yl]alkyl} amide derivatives have been designed and synthesized based on the structure and acitivity relationship (SAR) of phenylpiperazine series as α_1-adrenoceptor (α _1-AR) antagonists and the results of computer-aided drug design we studied before. All the target compounds have been identified by ~1H NMR, IR and MS (HRMS). Preliminary bioassay suggests that most of the target compounds display good blocking activity to α_1-AR. The potency (pA_2) of compound 3b is higher than prazosin.

Key words: PIPERAZINE P, ANTAGONIST, STRUCTURE ACTIVITY RELATIONSHIP, COMPUTER AIDED DESIGN, FURAN P, FORMIC ACID P, AMIDES P, BENZOPYRAN P, BIOLOGICAL ACTIVITY