Table of Contents
Metal-Based Drugs
Volume 5 (1998), Issue 6, Pages 323-332
http://dx.doi.org/10.1155/MBD.1998.323

Structure-Activity Relationships for Some Diamine, Triamine and Schiff Base Derivatives and Their Copper(II) Complexes

1Laboratory of Inorganic Chemistry, Dept. of Chemistry, Aristotle University of Thessaloniki, 54006, Greece
2Department of Physical and Theoretical Chemistry, University of Plovdiv, Plovdiv 4000, Bulgaria
3Institute of General and Inorganic Chemistry, Bulgaan Academy of Sciences, Sofia 1113, Bulgaria
4Laboratory of Biochemisty, Dept. of Chemistry, Aristotle University of Thessaloniki, 54006, Greece
5Theagenion Cancer Institute, Thessaloniki 54007, Greece

Received 7 October 1998; Accepted 20 October 1998

Copyright © 1998 Hindawi Publishing Corporation. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Ethylenediamine (en), putrescine (pu), diethylenetriamine (dien), dipropylenetriamine (dpta), spermidine (spmd) and their CuII compounds as well as the Schiff bases with 2-furaldehyde (dienOO), 2- thiophenecarboxaldehyde (dienSS) and pyrrole-2-carboxaldehyde (dienNN) of dien and that of dpta with 2- thiophenecarboxaldehyde (dptaSS), were prepared and characterised. They were tested against Bacillus substilis, Bacillus cereus, Staphylococcus aureus, Escherichia coli, Proteus vulgaris and Xanthomonas campestris as antibacterial reagents, the highest activity being exhibited by Cu(dptaSS)(NO3)2 complex, which acts as antibiotic. In the antiproliferative tests (vs. T47D,L929 and BHK21/c13 cell lines) the best results were obtained with Cu(dptaSS)2+ and Cu(dienSS)2+. Electronic structure calculations gave for dptaSS and dienSS the higher negative charges on the N atoms. The counter-ions (Br-, NO3- and SO42-) play an important role by modulating the reagent's selectivity versus the bacteria [Gram(+) or Gram(-)], but they have no effect on the antiproliferative activity.