[New isatin-derived hydrazones and Mannich bases with possible biological activity].
The paper presents a synthesis of six new Mannich bases, five hydrazones derived from 1-piperidino-methyl-5-R-isatin and three copper complex compounds of 3-(3'-R-phenyl-pyridazinil-hydrazone)-indoline-2-ones (R=H, CH3, OCH3). The structure of the new compounds was confirmed by the results of the elementary and spectral analysis. Pharmacodynamic studies indicated that copper complex compounds present effective biological properties. Thus, it can be seen that the experimental carrageenan-induced inflammatory oedema was 58.3% inhibited by the complex V (R=CH3) after oral administration. Antimicrobial tests revealed that only compound V (R=OCH3) shows a moderate antimicrobial activity against the gram-positive and gram-negative bacteria, used in the test.
Dorneanu
M
M
Facultatea de Farmacie, Universitatea de Medicină şi Farmacie Gr. T. Popa, Iaşi.
Stefănescu
E
E
Pavelescu
M
M
Păduraru
O
O
Aprotosoaie
C
C
Dănilă
C
C
Tuchiluş
C
C
D000818:Animals; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000494:pharmacology; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D002351:Carrageenan; D004353:Drug Evaluation, Preclinical; D006835:Hydrazones / Q000494:pharmacology* / Q000627:therapeutic use; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy; D007510:Isatin / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D008352:Mannich Bases / Q000494:pharmacology* / Q000627:therapeutic use; D051379:Mice; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000893:Anti-Inflammatory Agents; D006835:Hydrazones; D008352:Mannich Bases; D007510:Isatin; D002351:Carrageenan