Peptido-aminobenzophenones-Novel Open-ring Derivatives of 1, 4-Benzodiazepines

Abstract

A number of peptido-aminobenzophenones were prepared as ring-opened derivatives of 1, 4-benzodiazepines. These compounds were prepared from 2-aminobenzophenones, 2-aminobenzhydrols, or indoles and appropriate protedcted dipeptides or protected amino acids by coupling, oxidation (if necessary), and deprotection. Some title compounds had very high activities in antipentylenetetrazole and fighting tests in mice when orally administered. Very weak toxicity was also found in these compounds. Water solubility of peptido-aminobenzophenone salts and pH of their aqueous solution were also tested.