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Quantitative Stucture-Activity Relationship Studies on Calmodulin Antagonists of Alkylamino 1,2-Diphenylethvl-ene Compounds

Xiao-Ping Lei*, Chong-Hua Li, Hai-Zhen Zhong, G.Mrugacz, A.Sobieszek, R.E.Reid   

  1. 1. School of Pharmaceutical Sciences,Beijing Medical university, Beijing 100083;
    2. Institute of Molecular Biology Austrian Academy of Sciences, Salzburg, Austria;
    3. Faculry of Pharmaceutical Sciences, University of British Columbia, Vancouver, B.CCanadaV6T 1Z3
  • Received:1996-05-07 Revised:1996-09-11 Online:1996-12-15 Published:1996-12-15
  • Contact: Xiao-Ping Lei*

Abstract: 6-Amino-1.2-diphenylhex-1-ene is considered to be a new type of lead com-pound and structure-activity relationships for 15 calmodulin antagonists of alkylamino1.2-diphen-ylethylene compounds have been reported It has been found that the cis isomers generally show greate ractivity than the transisomers,and the reduced compound is the least active Inhibitory activity increases with the length of the alkyl chain separating the aromatic hydrophobic center from the basic center It is suggested from QSAR analysis that compounds Which have high hydrophobic parameter and with electron-donating substituents on the benzene ring may exhibit more potent in-hibitory activity.

Key words: Calmodulin antagonists, QSAR, Hansch analysis

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