Anthelmintic effects of alkylated diamines and amino alcohols against Schistosoma mansoni.

Polyamines are substances involved in many aspects of cell growth, division, and differentiation. Because of the metabolic differences between host cells and parasite cells, polyamine metabolism has been considered as a potential target for the chemotherapy of parasitic diseases. The aim of this work was to evaluate the schistosomicidal activity of different N-alkylated diamines (3a-3h), amino alcohols (4a-4d), and glycosylated amino alcohols (10a-10d). Compounds were prepared by synthetic methods and submitted to in vitro evaluation against adult worms of Schistosoma mansoni. At 100 µM, 3b, 3e, and 3h as well as 4a, 4b, 4d, 10a, 10b, and 10d resulted in 100% mortality of adult schistosomes. Compound 3d (12.5 to 100 µM) caused the death of 100% of both male and female adult schistosomes, while 3f (12.5 to 100 µM) resulted in 100% mortality of only male adult worms, whereas no mortality in female worms was observed. Compounds 3d and 3f were also able to reduce viability and decrease production of developed eggs in comparison with the negative control group. Diamines 3d and 3f may represent useful lead compounds for further optimization in order to develop new schistosomicidal agents.

Relationship between structure and antibacterial activity of lipophilic N-acyldiamines.

We report in this work the preparation and antibacterial evaluation of a series of N-monoacylated diamines against six Gram-positive and 11 Gram-negative bacteria. The results obtained showed the existence of relationship between lipophilicity and antibacterial activity of the tested compounds. The best results were obtained against Gram-positive bacteria for compounds having a 10-12 carbons alkyl chain. Compound 4e was the most active against Microccus lentus (MIC=2 microg/mL), Staphylococcus aureus ATCC 29213 (MIC=4 microg/mL) and Enterobacter aerogenes CDC 1680 (MIC=8 microg/mL).

Effect of vaccination and the immunomodulators "bacillus of Calmette-Guérin, avridine and Propionibacterium acnes" on rabies in mice.

Responses of vaccination and treatment to immunomodulators against rabies in mice were evaluated through macrophage inhibition factor (MIF), intra-pad inoculation (IPI) and serum neutralization (SN) tests and by the detection of gamma-interferon (IFN-gamma). Onco-BCG, Avridine and Propionibacterium acnes were administered to groups of mice. Higher survival rates were found in animals treated with P. acnes. Lower levels of IFN-gamma were observed in the groups of infected and vaccinated mice. The IPI was not effective on detecting the response of delayed-type hypersensitivity. Vaccine induced in the infected animals a more intense response to MIF reaction.