Ancistectorine D, a naphthylisoquinoline alkaloid with antiprotozoal and antileukemic activities, and further 5,8'- and 7,1'-linked metabolites from... (Publications)
the Chinese liana Ancistrocladus tectorius (Ancistrocladaceae), two new 5,8'-coupled naphthylisoquinolines, ancistectorine D (5) and its 6-O-demethyl derivative 6, were isolated, along with two new 7,1'-linked [...] (oxidative degradation) and chiroptical (circular dichroism) methods. Chemotaxonomically remarkable, 5,8'-coupled naphthylisoquinolines have as yet been found quite rarely in Asian Ancistrocladus species [...] coupling type represent the by far the largest group of constituents in...
Antiprotozoal dimeric naphthylisoquinolines, mbandakamines B3 and B4, and related 5,80'-coupled monomeric alkaloids, ikelacongolines A–D, from a... (Publications)
B4 (4), and four related 5,8′-linked monomeric alkaloids, named ikelacongolines A–D (5a, 5b, 6, and 7). The dimers 3 and 4 are structurally unusual quateraryls comprising two 5,8′-coupled monomers linked [...] were isolated from the here investigated Congolese liana, three of them belonging to the subclass of 5,8′-coupled naphthylisoquinoline alkaloids, whereas two compounds exhibited a less frequently occurring
A 5-year intervention study on elimination of urogenital schistosomiasis in Zanzibar: parasitological results of annual cross-sectional surveys (Publications)
interval (CI): 4.5%-7.6%) to 1.7% (95% CI: 1.2%-2.2%) in 9- to 12-year old students, from 3.9% (95% CI: 2.8%-5.0%) to 1.5% (95% CI: 1.0%-2.0%) in adults, and from 8.8% (95% CI: 6.5%-11.2%) to 2.6% (95% [...] public health problem from Pemba and to interrupt Schistosoma haematobium transmission from Unguja in 5 years. METHODOLOGY: A repeated cross-sectional cluster-randomized trial was implemented from 2011/12 [...] (95% CI: 1.7%-3.5%) in 1st year students from 2011/12 to 2017. In 2017, heavy...
Novel 1-methyl-1 <em>H</em>-pyrazole-5-carboxamide derivatives with potent anthelmintic activity (Publications)
the parasitic nematode Haemonchus contortus led to the identification of two 1-methyl-1 H-pyrazole-5-carboxamide derivatives. Medicinal chemistry optimization targeted modifications of the left-hand side
Modified 5'-trityl nucleosides as inhibitors of <em>Plasmodium falciparum</em> dUTPase (Publications)
discovery of 5'-tritylated analogues of deoxyuridine as selective inhibitors of this Plasmodium falciparum enzyme. Herein we report further structure-activity studies; in particular, variations of the 5'-trityl [...] ons of the base. Compounds were tested against both the enzyme and the parasite. Variations of the 5'-trityl group and of the 3'-substituent were well tolerated and yielded active compounds. However, there
Oxidative properties of ambient PM2.5 and elemental composition: Heterogeneous associations in 19 European cities (Publications)
extent to which constituents of PM2.5 (transition metals, sodium, chloride) contribute to the ability to generate hydroxyl radicals ((OH)-O-center dot) in vitro in PM2.5 sampled at 20 locations in 19 European [...] European centres participating in the European Community Respiratory Health Survey. PM2.5 samples (n = 716) were collected on filters over one year and the oxidative activity of particle suspensions obtained
Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives (Publications)
donovani and Trypanosoma brucei rhodesiense. N,N-Diethyl-5-((4-methoxyphenyl)imino)-5H-benzo[a]phenoxazin-9-amine shows IC(50)=0.040mumolL(-1) with a selective index of 1425 against Plasmodium falciparum K1 [...] A series of 5-phenyliminobenzo[a]phenoxazine derivatives were synthesized. The in vitro antiprotozoal activities were evaluated against Plasmodium falciparum K1, Trypanosoma cruzi, Leishmania donovani
Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds (Publications)
A small series of 5-nitro-2-aminothiazole-based amides containing arylpiperazine-, biphenyl- or aryloxyphenyl groups in their core were synthesized and evaluated as antitrypanosomatid agents. All tested