[Antiedematous activity of certain arylcarboxylate copper aquacomplexes].
Using rat paw carrageenan edema, the anti-inflammatory activity of nine selected arylcarboxylatocopper(II) aquacomplexes of the general composition Cu(RCOO)2.nH2O, where R represents 2-hydroxy-Y-methylphenyl, Y = 3 (n = 1.5), 4 (4) or 5 (2); 2-hydroxy-3,6-dimethylphenyl (n = 4); 2,5-diacetoxyphenyl (1); 2-methoxy-(1) and 4-methoxyphenyl (3); 2-furyl (3) and 2-thienyl (1), was assayed and compared to that of the free acids. Copper(II) salicylate tetrahydrate and salicylic acid were used as standards for comparison. All compounds were applied i.p. in a single dose of 50 mumol/kg body weight, calculated for the RCOO-fragment. m-Cresotato- (mean edema reduction 70%) and p-cresotatocopper(II) (80%) aquacomplexes were clearly more effective than copper(II) salicylate tetrahydrate (55%). The nonsubstituted hydroxyl of the salicylate skeleton of acidoligands is required for the activity of the complexes and of free acids tested. Isomeric cresotic acids (82-47-62%) and 2-furoic acid (48%) exhibited a higher effect than salicylic acid (42%). The relationship between the coordination-chemical properties and the biological effects of the complexes studied is discussed.
Sokolík
J
J
Katedra chemickej teórie lieciv a Katedra farmakológie a toxikológie Farmaceutickej fakulty Univerzity Komenského, Bratislava.
Tumová
I
I
Blahová
M
M
Harisová
E
E
Svec
P
P
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000627:therapeutic use*; D002351:Carrageenan; D003300:Copper; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D009942:Organometallic Compounds / Q000737:chemistry / Q000627:therapeutic use*; D051381:Rats; D012459:Salicylates / Q000627:therapeutic use; D020156:Salicylic Acid
D000893:Anti-Inflammatory Agents; D009942:Organometallic Compounds; D012459:Salicylates; D003300:Copper; D002351:Carrageenan; D020156:Salicylic Acid
Antiedematózna aktivita vybraných arylkarboxylátomednatých akvakomplexov.