Prodn. of bifunctional Schiff base chelating agents - and copper complexes useful as antirheumatic and antitumour agents

摘要

Prepn of a di-Schiff base coordinated Cu complex (I) and apo chelator comprises reacting: (a) an aliphatic diamine or a di-aldehyde or -ketone (pref of 3-6 and esp 4C atoms); and (b) a heterocyclic aldehyde or amine (pref contg S, 0 or esp N); in a protic or aprotic medium at neutral or alkaline pH, opt in presence of inorganic Cu salts. USE/ADVANTAGE - (I) is useful as an anti-rheumatic and anti-tumorigenic agent. It is active against the prodn of eg PMNs and Macrophages and is therefore useful for mopping up superoxide and hydroxyl radicals. In an example, a rat model of rapid-proliferating Walker carcinosarcoma 256 was administered with the di-Schiff complex and remission rates of 75% and 60% were observed for intratumour and intravenous injections respectively.