Estimation of the lipophilicity of antiarrhythmic and antihypertensive active 1‐substituted pyrrolidin‐2‐one and pyrrolidine derivatives | Zendy

Kulig Katarzyna | Zendy; Malawska Barbara | Zendy

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Estimation of the lipophilicity of antiarrhythmic and antihypertensive active 1‐substituted pyrrolidin‐2‐one and pyrrolidine derivatives

Author(s) -

Kulig Katarzyna,

Malawska Barbara

Publication year - 2003

Publication title -

biomedical chromatography

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.4

H-Index - 65

eISSN - 1099-0801

pISSN - 0269-3879

DOI - 10.1002/bmc.246

Subject(s) - lipophilicity , chemistry , partition coefficient , chromatography , high performance liquid chromatography , pyrrolidine , acetonitrile , reversed phase chromatography , stereochemistry

The lipophilicity of some antiarrhythmic and antihypertensive active 1‐[2‐hydroxy‐ or 1‐[2‐acetoxy‐3‐(4‐aryl‐1‐piperazinyl)propyl]pyrrolidin‐2‐one derivatives ( 1 – 12 ) has been investigated. Their lipophilicity ( R MO and log k ′) was determined by reversed‐phase thin‐layer chromatography and reversed‐phase high‐performance liquid chromatography with mixtures of acetonitrile and Tris buffer as mobile phases. The partition coefficients of compounds 1 – 12 (log P ScilogP ) were also calculated with the ScilogP program. Comparison of R MO , log k ′ and calculated log D 7.0 ScilogP values enabled calculation of clog D 7.0 TLC and clog D 7.0 HPLC values. Preliminary quantitative structure–activity relationship studies indicated that for active compounds there is a dependence between affinity for α 2 ‐adrenoceptors and their clog D 7.0 HPLC values. Copyright © 2003 John Wiley & Sons, Ltd.

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