Antihemolytic, antiproteolytic and anticonvulsant properties of 10-substituted hydrazonoacetyl phenothiazines.
Twelve 10-substituted hydrazonoacetyl phenothiazines were synthesized, characterized and evaluated for their antihemolytic, antiproteolytic and anticonvulsant properties. The degree of protection of the in vitro hypoosmotic hemolysis of human red blood cells by these compounds ranged from 30-65%, at a final concentration of 1 mM. All phenothiazine derivatives (1 mM) possessed antiproteolytic activity which was reflected by 25-71% protection observed with these compounds against in vitro trypsin-induced hydrolysis of bovine serum albumin. These compounds at a dose of 100 mg/kg provided 20-80% protection against pentylenetetrazol-induced convulsions in mice. All phenothiazine derivatives possessed low toxicity which was reflected by their approximate LD50 values ranging from 500- greater than 1000 mg/kg.
D000818:Animals; D000927:Anticonvulsants; D005260:Female; D006461:Hemolysis / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D010640:Phenothiazines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D014361:Trypsin Inhibitors
D000927:Anticonvulsants; D010640:Phenothiazines; D014361:Trypsin Inhibitors