[The reaction of 3-(R-phenyl)-6-hydrazine pyridazines with substituted isatins (II)].
This paper presents the synthesis of six hydrazones from isatin and 1-morpholinomethyl-isatin and also of their six cooper's complex salts. Their structure was confirmed by the results of the quantitative elemental analysis and by IR, UV-VIS spectral analysis. The biological tests point out that cooper's complex salt of 3-(3'-phenyl-pyridazinylhydrazono)-5-methyl-indoline-2-one (1:2) (VI a) has the smallest toxicity (DMT over 800 mg/kg.w. p.o.), a remarkable anti-inflammatory activity (inhibition 57.1%, IAR 1.1) and also a gastroprotector coefficient of 43.3%. In the mean time, the cooper's complex salt of 3-(3'-p-anisyl-pyridazinyl-hydrazono)-5-methyl-ind oline-2-one (1:2) (VI b) has a gastroprotector coefficient of 76.3% and a lower anti-inflammatory activity than the first derivative (inhibition 36.9%).
Dorneanu
M
M
Faculté de Pharmacie, Université de Médecine et de Pharmacie Gr. T. Popa, Iaşi.
Stefănescu
E
E
Pavelescu
M
M
Hriscu
A
A
Alexandrescu
C D
CD
Gherase
F
F
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D002351:Carrageenan; D004353:Drug Evaluation, Preclinical; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005260:Female; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy; D007510:Isatin / Q000031:analogs & derivatives* / Q000737:chemistry; D008297:Male; D051379:Mice; D011724:Pyridazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity
D000893:Anti-Inflammatory Agents; D011724:Pyridazines; D007510:Isatin; D002351:Carrageenan