Benzylpiperazine derivatives. IX. Structure-antiulcer activity studies of 1-(aminocarbonylalkyl)-4-benzylpiperazine derivatives by the adaptive least-squares method.

doi:10.1248/CPB.36.3955

Paper

Benzylpiperazine derivatives. IX. Structure-antiulcer activity studies of 1-(aminocarbonylalkyl)-4-benzylpiperazine derivatives by the adaptive least-squares method.

Published Oct 25, 1988 · H. Ohtaka, K. Yoshida, K. Suzuki

Chemical & pharmaceutical bulletin

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Abstract

Quantitative structure-antiulcer activity relationships of 1-(aminocarbonylalkyl)-4-benzylpiperazine derivatives (I) were analyzed by using the adaptive least-squares (ALS) technique. Discriminant functions show that (1) a bulky amide moiety is disadvantageous, (2) a small number of methylene groups between carbonyl and piperazine is favorable, (3) a substituent which has a large B1 value (or B2 value when the substituent is forced to be in the in-plane conformation) with low lipophilicity at the 3 and/or 4 position of the benzyl moiety is favorable for antiulcer activity with low acute toxicity.

Study Snapshot

A small number of methylene groups between carbonyl and piperazine is favorable for antiulcer activity, while a large B1 value with low lipophilicity at the 3 and/or 4 positions of the benzyl moiety is favorable for low acute toxicity.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Benzylpiperazine derivatives. IX. Structure-antiulcer activity studies of 1-(aminocarbonylalkyl)-4-benzylpiperazine derivatives by the adaptive least-squares method.

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