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The syntliesis of dibenzo [b,e] [l,.l]diazepines substituted in the 5-and IO-positions with dialkylaminonlkyl groups :mtl tlieir wtivitv ns pseudocholinesterase inhibitors are reported.In 1924 Clemo, Perkin, and Robinson1 reported the synthesis of 1 la-dibenzo [b,e] [1,4]diazepin-ll-one (I) by the pyrolysis of ?;-(o-aminophenyl)aJlthraIlilic acid. R4

Water-soluble derivatives of ara-cytidine (cytarabine, Cytosar) were prepared and tested for antitumor, immunosuppressive, and antiarthritic activities in animals after oral administration. The compounds tested included the 5'-palmitate, 5'-benzoate, and 5'-adamantoate esters of ara-cytidine, made water soluble by use of their hydrochloride salts of peptidyl derivatives, and two basic 5' esters (5'-nicotinoate and 5'-quinuclidinate) as their hydrochloride salts. Five of the compounds had antitumor activity superior to that found with ara-cytidine itself after oral administration in the L1210 leukemic mouse assay. One of these, 5'-adamantoyl-ara-cytidine hydrochloride, had antitumor activity after oral administration approaching that achieved with parenterally administered ara-cytidine.

The APS Journal Legacy Content is the corpus of 100 years of historical scientific research from the American Physiological Society research journals. This package goes back to the first issue of each of the APS journals including the American Journal of Physiology, first published in 1898. The full text scanned images of the printed pages are easily searchable. Downloads quickly in PDF format.