Synthesis and antipsychotic activity of conformationally constrained 'tripeptoid' neurotensin analogues

摘要

Recently we developed a series of "tripeptoid" analogues of neurotensin (NT) with antipsychotic activity [1,2].Their conformational properties ahve been investigated in solution by IR and NMR spectroscopy and the experiments indicated their favored conformational states in this condition are the beta-folding modes.The spectroscopy-derived molecular models are very similar to those established by theoretical calculations and analyses.Now we synthesized the NT analogues containing betaI-,betaII-and betaII'-turn constraints.