[Synthesis and biological properties of 3,5-cyclophosphates- and -amidophosphates of 1,2-O-alkylydene-6-deoxy-6-halogeno-alpha -D-glucofuranoses]. / Sintez i biologicheskie svoistva 3,5-tsiklofosfatov i amidofosfatov 6-galoid-6-dezoksi-1,2-O-alkiliden-alpha-D-gliukofuranoz.

3,5-Cyclic phosphates and phosphoramides of 6-halogenated glucofuranoses were synthesized via interaction of 3,5,6-bicyclophosphites of 1,2-O-alkylidene-alpha-D-glucofuranoses with halogens (followed by treatment with nucleophilic reagents) and N-chloroamines. 3,5-Cyclic trans-dibutylphosphoramides of 6-chloro-6-deoxy-1,2-O-isopropylidene- and 6-chloro-6-deoxy-(R)-(2,2,2)-trichloroethylidene)-alpha-D-glucofuranoses were shown to possess antiproliferative activity against CaOv human ovarian carcinoma cells in vitro (CE50 of approximately 10(-5) M). Cyclic trans-dibutylphosphoramide of 6-chloro-6-deoxy-1,2,-O-isopropylidene-alpha-D-glucofuranose also displayed marked antitumor effect on P-388 transplantable murine leukemia in vivo (the maximum increase in life span of 100% was reached at the quintuple injection of 100 mg/kg daily).

[Improvement of the therapeutic efficacy of fosfomycin by addition of glucose-6-phosphate in the treatment of intraperitoneally infected mice (author's transl)]. / Wirkungssteigerung von Fosfomycin durch Zusatz von Glukose-6-Phosphat bei intraperitoneal infizierten Mäusen.

The increase of antimicrobial activity of Fosfomycin by glucose-6-phosphate (G-6-P) has often been demonstrated by in vitro studies. However, this effect was never sufficiently established in vivo. Our study was carried out in order to investigate the effects of the addition of G-6-P to Fosfomycin in white mice (strain G.P. of N.I.H.), which were intraperitoneally infected with a strain of S. typhimurium (10(3) c.f.u/0.5 ml i.p.). One and six hours after the infection, 0.1 ml consisting of increasing doses of G-6-P (0, 5, 25, 50, 250 and 500 micrograms/g) and decreasing doses of Fosfomycin (15.6, 7.8, 3.9, 1.95, 0.98 and 0.49 micrograms/g) were applied i.m., using 10 animals for each combination. Tables 1 and 2 show the results of this therapy with regard to the reduction of the ED50 of Fosfomycin. It can be seen that the addition of 25 micrograms G-6-P/g body-weight significantly reduces the ED50 within the first days (Tab. 1), while doses of 50 and more micrograms G-6-P/g significantly reduce the ED50 during the whole investigation period (Tab. 2). These results justify the proposal to use a combination of Fosfomycin and G-6-P in clinical studies for the treatment of human infections.

[Trial of a combination of proscillaridin A, thioridazine and Cori ester in the ambulatory treatment of some cardiopathies, especially senile types]. / Sperimentazione di una associazione di proscillaridina A, tioridazina ed estere di Cori nel trattamento ambulatoriale di alcune cardiopatie in particolare senili

The effect of an association of proscillaridin A, thioridazine and Cori ester in ambulatory management of certain heart diseases, particularly in aged subjects, was assessed. Satisfactory results were observed in 58.3% of cases, with significant improvement of cardiac erethism, psychomotor instability and sleep disturbances, as well as cardiac frequency and signs of myocardial insufficiency. It is felt that the association is of assistance in the treatment of certain heart diseases unaccompanied by frank signs of insufficiency, especially in aged subjects.