59179-94-1Relevant academic research and scientific papers
Peptidoaminobenzophenones, a novel class of ring-opened derivatives of 1,4-benzodiazepines
Hirai,Ishiba,Sugimoto,Sasakura,Fujishita,Toyoda,Tsukinoki,Joyama,Hatakeyama,Hirose
, p. 764 - 773 (2007/10/02)
A series of novel peptidoaminobenzophenones has been prepared via several routes and was evaluated for CNS activity. The structure-activity relationships in the series are discussed. In general, dipeptido-N-methylaminobenzophenones showed higher activities than the corresponding NH derivatives. Some compounds had very high activities in antipentylenetetrazole and antifighting tests in mice when orally administered. Very weak toxicity was also found in these compounds. Water solubility of the peptidoaminobenzophenones and their salts were tested. Possible in vivo conversion of peptidoaminobenzophenone by enzymatic cleavage of the terminal amino acid, followed by chemical cyclization to 1,4-benzodiazepine, is also discussed. Such novel open-ring derivatives of 1,4-benzodiazepine may serve as useful CNS agents.
Dipeptide derivatives and their production
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, (2008/06/13)
Dipeptide derivatives represented by the formula: STR1 wherein R represents hydrogen, C1 -C6 alkyl group, C2 -C7 alkenyl group, C2 -C7 cyanoalkyl group, C2 -C7 carbamoylalkyl group, C3 -C10 dialkylaminoalkyl group or cyclopropylmethyl group, R1 represents hydrogen, C1 -C6 alkyl group, C7 -C14 aralkyl group, C7 -C14 hydroxyaralkyl group, C6 -C12 aryl group, C2 -C7 carbamoylalkyl group, C2 -C7 carboxyalkyl group, C1 -C6 aminoalkyl group, C4 -C10 guanidylalkyl group, C1 -C6 mercaptoalkyl group, C2 -C7 alkylthioalkyl group, C9 -C15 indolylalkyl group or C4 -C9 imidazolylalkyl group, R2 represents hydrogen, C1 -C6 alkyl group, C7 -C14 aralkyl group, C6 -C12 aryl group, glycyl group or glycyl-glycyl group, R3 represents hydrogen, C1 -C6 alkyl group or amino-protecting group, R1 and R2 optionally combine to from C2 -C4 alkylene group, group R2 --N--R3 optionally represents phthalimido group, piperidino group, 4-hydroxy-4-(p-halogenophenyl)piperidino, morpholino, or piperazino group substituted by C1 -C6 alkyl group or phenyl group, A ring represents benzene ring or pyridine ring optionally substituted by halogen and B ring represents benzene ring or thiophene ring optionally substituted by halogen, trifluoromethyl group, methylsulfonyl group, nitro group or C1 -C6 alkyl group and their acid addition salts, being useful as anxiolytics, sedatives, anticonvulsants, hypnotics, muscle relaxants, or their synthetic intermediates, are prepared.
