Anthelmintic Effects of Alkylated Diamines and Amino Alcohols againstSchistosoma mansoni

Abstract

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.

Anthelmintic Activity of Crude Extract and Essential Oil ofTanacetum vulgare(Asteraceae) against Adult Worms ofSchistosoma mansoni

“…The presence of S. mansoni eggs in the host tissues has been reported to be closely related to the pathology of human schistosomiasis [ 12 , 20 ]. The permanent pairing of the schistosomes couples in the blood system of their hosts vertebrates throughout their lifespan causes high rate of oviposition, which is responsible for the resulting immunopathological lesions, characterized by inflammation and fibrosis in the target [ 13 ].…”

“…On the basis of the folkloric uses of T. vulgare as an anthelmintic and a vermifuge, as well as in continuation of our search for active natural sources against S. mansoni [ 20 – 24 ], the present study evaluated the in vitro schistosomicidal effects of the extract and the essential oil of T. vulgare , which have not yet been described.…”

Synthesis and Antibacterial Activity of Alkylated Diamines and Amphiphilic Amides of Quinic Acid Derivatives

“…Synthesis N-alkylated diamines 2a-h were prepared in 65-85% yield by nucleophilic substitution reaction between diamines 1a-d with decyl chloride or dodecyl chloride in ethanol under reflux, as previously reported (Scheme 1) (10)(11)(12)14,24,25).…”

Mechanisms of Action of Substituted β-Amino Alkanols on Leishmania donovani

“…␤-Amino alkanols have consistently demonstrated their usefulness as new lead compounds against protozoan diseases (12,28,29), including those caused by Leishmania spp. (15,30) and Trypanosoma brucei brucei (31).…”

“…Nevertheless, in the long term, the development of new leads is mandatory in order to hasten their optimization and further implementation. ␤-Amino alkanols, chemically derived from ␣-amino acids by reduction, display considerable pharmacological versatility, having been successfully tested as anti-inflammatory, antitumor, antibiotic, or adjuvant agents, among others (10)(11)(12)(13). Proof of concept for their use as leishmanicidal agents has been also reported (13)(14)(15).…”