A5084123396- Trypanosoma species research and implications
- Research on Leishmaniasis Studies
- Synthesis and Biological Evaluation
- Malaria Research and Control
- Traditional and Medicinal Uses of Annonaceae
- Synthesis and biological activity
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Phytochemical compounds biological activities
- Biochemical and Molecular Research
- Microbial Natural Products and Biosynthesis
- Natural product bioactivities and synthesis
- Phenothiazines and Benzothiazines Synthesis and Activities
- Bioactive Compounds and Antitumor Agents
- Insect Pest Control Strategies
- HIV/AIDS drug development and treatment
- Marine Sponges and Natural Products
- Synthesis and Catalytic Reactions
- Toxin Mechanisms and Immunotoxins
- Chemical Synthesis and Analysis
- Entomopathogenic Microorganisms in Pest Control
- Axial and Atropisomeric Chirality Synthesis
- Quinazolinone synthesis and applications
- Carbohydrate Chemistry and Synthesis
- Phytochemistry and Biological Activities
Swiss Tropical and Public Health Institute
2016-2025
University of Basel
2016-2025
Frankfurt School of Finance & Management
2021
University of Bern
2020
Johns Hopkins University
2020
Biology of Infection
2017
University of Dundee
2016
Goethe University Frankfurt
2015
University of Graz
2005-2014
Swiss School of Public Health
2012-2014
ABSTRACT Trypanosomiasis and leishmaniasis are important parasitic diseases affecting millions of people in Africa, Asia, South America. In a previous study, we identified several flavonoid glycosides as antiprotozoal principles from Turkish plant. Here surveyed large set aglycones glycosides, well panel other related compounds phenolic phenylpropanoid nature, for their vitro activities against Trypanosoma brucei rhodesiense , cruzi Leishmania donovani . The cytotoxicities more than 100...
Background Human African trypanosomiasis (HAT), also known as sleeping sickness, is a fatal parasitic disease caused by trypanosomes. Current treatment options for HAT are scarce, toxic, no longer effective, or very difficult to administer, in particular the advanced, stage of (stage 2, chronic HAT). New safe, effective and easy-to-use treatments urgently needed. Here it shown that fexinidazole, 2-substituted 5-nitroimidazole rediscovered Drugs Neglected Diseases initiative (DNDi) after...
Background Human African trypanosomiasis (HAT) is an important public health problem in sub-Saharan Africa, affecting hundreds of thousands individuals. An urgent need exists for the discovery and development new, safe, effective drugs to treat HAT, as existing therapies suffer from poor safety profiles, difficult treatment regimens, limited effectiveness, a high cost goods. We have discovered optimized novel class small-molecule boron-containing compounds, benzoxaboroles, identify SCYX-7158...
We report in this paper an evolutionary experiment on Drosophila that tested life-history theory and the of aging. As predicts, higher extrinsic mortality rates did lead to evolution intrinsic rates, shorter lifespans, decreased age size at eclosion; peak fecundity also shifted earlier life. These results confirm key role growth, maturation, reproduction, aging, they do so with a selection regime maintained fertility throughout life while holding population densities constant.
In this study, thirteen sponge-derived terpenoids, including five linear furanoterpenes: furospinulosin-1 (1), furospinulosin-2 (2), furospongin-1 (3), furospongin-4 (4), and demethylfurospongin-4 (5); four meroterpenes: 2-(hexaprenylmethyl)-2-methylchromenol (6), 4-hydroxy-3-octaprenylbenzoic acid (7), 4-hydroxy-3-tetraprenyl-phenylacetic (8), heptaprenyl-p-quinol (9); a triterpene, squalene (10); two spongian-type diterpenes dorisenone D (11) 11 beta-acetoxyspongi-12-en-16-one (12);...
Slipped under the radar? 1H NMR spectroscopic examination revealed that [Ru(η6-arene)Cl2(L)] (L=N-heterocyclic ligands) complexes readily undergo a ligand exchange reaction in DMSO (see scheme), popular medium for preparing stock solutions biological screening. It is therefore highly important researchers to study stability before reporting on activity of such complexes.
Fexinidazole is a 5-nitroimidazole drug currently in clinical development for the treatment of human sleeping sickness (human African trypanosomiasis [HAT]), caused by infection with species protozoan parasite Trypanosoma brucei. The compound and its two principal metabolites, sulfoxide sulfone, have been assessed their ability to kill range T. brucei strains vitro cure both acute chronic HAT disease models mouse. parent molecule metabolites shown trypanocidal activity 0.7-to-3.3 μM...
Chemical investigation of the dichloromethane root extract Waltheria indica led to isolation and characterization 10 quinoline alkaloids, namely, 8-deoxoantidesmone (1), waltheriones E–L (2–9), antidesmone (10). Among these, compounds 2–9 have not yet been described in literature. Their chemical structures were established by means spectroscopic data interpretation including 1H 13C NMR, HSQC, HMBC, COSY, NOESY experiments UV, IR, HRESIMS. The absolute configurations comparison experimental...
Neglected tropical diseases cause significant morbidity and mortality are a source of poverty in endemic countries. Only few drugs available to treat such as leishmaniasis, Chagas’ disease, human African trypanosomiasis malaria. Since drug development is lengthy expensive, repurposing strategy offers an attractive fast-track approach speed up the process. A set 100 registered with repositioning potential for neglected was assembled tested vitro against four protozoan parasites associated...
Abstract Exchange of the native promoter to arabinose‐inducible P BAD was established in entomopathogenic bacteria silence and/or activate gene clusters involved natural product biosynthesis. This allowed “on‐demand” production GameXPeptides, xenoamicins, and blue pigment indigoidine. The for novel “mevalagmapeptides” highly toxic xenorhabdins were identified by this approach.
Millions who live in Latin America and sub-Saharan Africa are at risk of trypanosomatid infections, which cause Chagas disease human African trypanosomiasis (HAT). Improved HAT treatments available, but therapies rely on two nitroheterocycles, suffer from lengthy drug regimens safety concerns that frequent treatment discontinuation. We performed phenotypic screening against trypanosomes identified a class cyanotriazoles (CTs) with potent trypanocidal activity both vitro mouse models HAT....
The Experimental Natural Products Knowledge Graph (ENPKG) framework combines a sample-centric approach with semantic enrichment to organize large heterogeneous metabolomics data sets as knowledge graph. Harmonization of experimental publicly available and federated queries mechanisms enable efficient information extraction the contextualization studies, thereby offering exciting opportunities for drug discovery global chemodiversity characterization.
Abstract Canalization describes the process by which phenotypic variation is reduced developmental mechanisms. A trait can be canalized against environmental or genetic perturbations. Stabilizing selelction should favor improved canalization, and degree of a trait's canalization positively correlated with its impact on fitness. Here we report, for Drosophila melanogaster , measurements five fitness components. We compare them discuss inbreeding both. In three experiments measured components...
Aerucyclamides C and D were isolated from the cyanobacterium Microcystis aeruginosa PCC 7806, their structures established by NMR spectroscopy chemical transformation degradation. Acidic hydrolysis of aerucyclamide (CF3CO2H, H2O) resulted in microcyclamide 7806A. This evidence combined with spectroscopic physical data suggest a structure revision for 7806A, which incorporates an O-acylated Thr ammonium residue instead originally proposed methyl oxazoline ring. We have prepared 7806B upon...
In the present study,13 bromopyrrole alkaloids, including oroidin analogs hymenidin (2), dispacamide B (3) and D (4), stevensine (5) spongiacidin (6), their derivatives lacking imidazole ring bromoaldisin (7), longamide (8) A (9), dimeric sceptrin (10) dibromopalau’amine (11), non-oroidin bromopyrrolohomoarginin (12), manzacidin (13), agelongine (14), obtained from marine sponges belonging to Axinella Agelas generahave been screened in vitro against four parasitic protozoa, i.e., two...
Prompted by results of our previous studies where we found high activity some sesquiterpene lactones (STLs) against Trypanosoma brucei rhodesiense (which causes East African sleeping sickness), have now conducted a structure-(in-vitro)-activity study on set 40 STLs T. rhodesiense, cruzi, Leishmania donovani and Plasmodium falciparum. Furthermore, cytotoxic L6 rat skeletal myoblast cells was assessed. Some the compounds possess activity, especially (e.g. helenalin its esters with IC50-values...
A novel class of antimalarial pyrido[1,2-a]benzimidazoles were synthesized and evaluated for antiplasmodial activity cytotoxicity following hits identified from screening commercially available compound collections. The most active these, TDR86919 (4c), showed improved in vitro vs the drug-resistant K1 strain Plasmodium falciparum relative to chloroquine (IC(50) = 0.047 μM v 0.17 μM); potency was retained against a range drug-sensitive strains, with negligible mammalian (L-6) cell line...
ABSTRACT We report the discovery of novel boron-containing molecules, exemplified by N -(1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)-2-trifluoromethylbenzamide (AN3520) and 4-fluoro- (SCYX-6759), as potent compounds against Trypanosoma brucei in vitro , including two subspecies responsible for human disease T. b. rhodesiense gambiense. These oxaborole carboxamides cured stage 1 (hemolymphatic) trypanosomiasis infection mice when administered orally at 2.5 to 10 mg/kg body weight 4...
A series of novel 3-nitro-1H-1,2,4-triazole-based (and in some cases 2-nitro-1H-imidazole-based) amides and sulfonamides were characterized for their vitro antitrypanosomal antileishmanial activities as well mammalian toxicity. Out 36 compounds tested, 29 (mostly 3-nitro-1H-1,2,4-triazoles) displayed significant activity against Trypanosoma cruzi intracellular amastigotes (IC(50) ranging from 28 nM to 3.72 μM) without concomitant toxicity L6 host cells (selectivity 66-2782). Twenty-three...
A series of 75 guanidine and 2-aminoimidazoline analogue molecules were assayed in vitro against Trypanosoma brucei rhodesiense STIB900 Plasmodium falciparum K1. The dicationic diphenyl compounds exhibited the best activities with IC50 values T. b. P. nanomolar range. Five (7b, 9a, 9b, 10b, 14b) cured 100% treated mice upon ip administration at 20 mg/kg difficult to cure mouse model. Overall, that bear cations benefit from better safety profiles than counterparts. observation a correlation...
In a screen of 880 extracts from plants and fungi for antiplasmodial, antitrypanosomal, leishmanicidal activity, an ethyl acetate extract the mushroom Ganoderma lucidum showed antiplasmodial activity with 79% inhibition at 4.9 μg/mL. HPLC-based profiling subsequent isolation compounds yielded seven lanostanes (1−7), which three (2, 3, 7) were new. A new benzofuran derivative (8) farnesyl hydroquinone ganomycin B was also identified. The structures relative configurations elucidated by...