Benzylpiperazine Derivatives. X. Syntheses and Structure-Antiulcer Activity Relationship of 1-Benzy1-4-piperazineacetic Acid Esters

HIROSHI OHTAKA; KENJI YOSHIDA; KENJI SUZUKI; KOICHI SHIMOHARA; SHIGERU TAJIMA; KEIZO ITO

doi:10.1248/cpb.36.4825

HIROSHI OHTAKA, KENJI YOSHIDA, KENJI SUZUKI, KOICHI SHIMOHARA, SHIGERU TAJIMA, KEIZO ITO

著者情報

キーワード: benzylpierazine derivative, 1-piperazineacetate, quantitative structure-activity relationship, ALS method, antiulcer activity

ジャーナルフリー

1988 年 36 巻 12 号 p. 4825-4833

DOI https://doi.org/10.1248/cpb.36.4825

詳細

抄録

A series of ester derivatives of1-benzy1-4-piperazineacetic acid was synthesized and evaluated as antiulcer agents. Quantitative structure-activity relationships (QSAR) analyses by using the ALS (adaptive least-squares) method were performed in each step to decrease the synthetic efforts. The QSAR for the esters is much the same as that for the previously examined amide derivatives. The antiulcer activity of these compounds was considered to be based on the cytoprotective activity. The most active and the least toxic compounds, 5n and 5y, were selected for further study.

責任著者(Corresponding author)

J-STAGEへの登録はこちら（無料）