The objective of this study was to prepare hyoscine butylbromide (a drug with bitter taste) tablets that can rapidly disintegrate in saliva. The granules were prepared by the extrusion method using aminoalkyl methacrylate copolymers (Eudragit E-100). The drugs dissolved rapidly in medium at pH 1.2 in a dissolution test while none of the drugs dissolved from the granules (% of dissolved < 5%) ev...

synthesized from dipeptidyl chloromethyl ketones or methyl ketones. According to this novel procedure, various functional groups could be introduced into positions 3 and 6 of 1,2-dihydropyrazin-2-one by using appropriate amino acids (Chart 2). It had been assumed that the formation of the 1,2-dihydropyrazin-2-one ring from dipeptidyl chloromethyl ketones proceeded according to the mechanism sho...

Following our previous investigations on certain new aminoalkyl aryl ethers, which showed promising and outstanding local anaesthetic properties, the local anaesthetic activity and duration of action of a further selection of four novel derivatives of the above-mentioned series, used as hydrochloride salts, have been determined by the ill vivo rat sciatic nerve test. These are: N,N-dimethyl...

The acute intravenous toxicities of a selection of three potential long-acting local anaesthetics belonging to the series of2- phenoxyethyldialkylamine were determined in mice. Two of the compounds were tertiary amines and the third a quaternary ammonium derivative.The I.V. median lethal dose, (LDso) of one of the tertiary compounds, 21A [N, N- diethyl-2- (2,6- diisopropyl) ethyl amine hyd...

Recently, using structure-inspired drug design, we demonstrated that aminoalkyl derivatives of beta-cyclodextrin inhibited anthrax lethal toxin action by blocking the transmembrane pore formed by the protective antigen (PA) subunit of the toxin. In the present study, we evaluate a series of new beta-cyclodextrin derivatives with the goal of identifying potent inhibitors of anthrax toxins. Newly...

A series of 2-aminoalkyl-5-nitropyrazolo[3,4,5-kl]acridines (pyrazoloacridines) was evaluated in vitro for activity against a panel of human tumor cell lines of breast, colon, or lung origin. Several pyrazoloacridines were found to possess solid tumor selectivity relative to their activity against murine leukemia L1210 cells as well as human lymphoblastoid cells. The superior compounds in this ...