Acyl derivatives of 1,5-benzodiazepines. III. Acyl derivatives of ethyl ester of 4-methyl-1H-tetrahydro-1,5-benzodiazepine-2-carboxylic acid

Pol J Pharmacol Pharm. 1988 Sep-Oct;40(5):471-80.

Abstract

Two series of derivatives of ethyl ester of 4-methyl-1H-tetrahydro-1,5-benzodiazepine-2-carboxylic acid (1) have been synthesized. The acetyl derivative (2) of ester 1 in preliminary pharmacological screening showed analgesic activity in the "writhing" test and the benzoyl derivative (5) exhibited antianxiety properties in the four plate test, while N,N-disubstituted aminoacetyl derivatives of 1 showed analgesic and anticonvulsant activity (10).

MeSH terms

  • Analgesics
  • Animals
  • Anticonvulsants
  • Apomorphine / pharmacology
  • Behavior, Animal / drug effects*
  • Benzodiazepines / chemical synthesis*
  • Benzodiazepines / pharmacology
  • Benzodiazepines / toxicity
  • Chemical Phenomena
  • Chemistry
  • Female
  • Lethal Dose 50
  • Male
  • Mice
  • Rats
  • Reserpine / antagonists & inhibitors
  • Serotonin Antagonists
  • Stereotyped Behavior / drug effects

Substances

  • Analgesics
  • Anticonvulsants
  • Serotonin Antagonists
  • Benzodiazepines
  • Reserpine
  • Apomorphine