ArticleAntimicrobial agents and chemotherapy2015
Activities of N,N'-Diarylurea MMV665852 analogs against Schistosoma mansoni.
Article in Antimicrobial agents and chemotherapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed.
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- Structure activity relationships of antischistosomalResults in chemistry · 2024Article
- Direct additive-free N-formylation and N-acylation of anilines and synthesis of urea derivatives using green, efficient, and reusable deep eutectic solvent ([ChCl][ZnClScientific reports · 2024Article
- Activity of N-phenylbenzamide analogs against the neglected disease pathogen, Schistosoma mansoni.Bioorganic & medicinal chemistry letters · 2023Article
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- The Different Facets of Triclocarban: A Review.Molecules (Basel, Switzerland) · 2021Review
- Activities of Quinoxaline, Nitroquinoxaline, and [1,2,4]Triazolo[4,3-a]quinoxaline Analogs of MMV007204 against Schistosoma mansoni.Antimicrobial agents and chemotherapy · 2021Article
- Diarylureas: Repositioning from Antitumor to Antimicrobials or Multi-Target Agents against New Pandemics.Antibiotics (Basel, Switzerland) · 2021Review
- Protein Kinases: Potential Drug Targets AgainstFrontiers in cellular and infection microbiology · 2021Review
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- Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?RSC medicinal chemistry · 2020Review
- Pentafluorosulfanyl-containing Triclocarban Analogs with Potent Antimicrobial Activity.Molecules (Basel, Switzerland) · 2018Article
- Identification of di-substituted ureas that prevent growth of trypanosomes through inhibition of translation initiation.Scientific reports · 2018Article
- Progress in antischistosomal N,N'-diaryl urea SAR.Bioorganic & medicinal chemistry letters · 2018Article
- Impedance-based detection ofIEEE Biomedical Circuits and Systems Conference : healthcare technology : [proceedings]. IEEE Biomedical Circuits and Systems Conference · 2017Article
- Controlling schistosomiasis with praziquantel: How much longer without a viable alternative?Infectious diseases of poverty · 2017Review
- Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond.PLoS pathogens · 2016Article
- Repurposing of anticancer drugs: in vitro and in vivo activities against Schistosoma mansoni.Parasites & vectors · 2015Article
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Authors and funding
7 authors.
Funding
Abstract
There is an unmet need to discover and develop novel antischistosomal drugs. As exemplified by MMV665852, N,N'-diarylureas have recently emerged as a promising antischistosomal chemotype. In this study, we evaluated the structure-activity relationships of 46 commercially available analogs of MMV665852 on newly transformed schistosomula (NTS) and adult Schistosoma mansoni worms in vitro. Active compounds were evaluated with a cytotoxicity assay, in silico calculations, metabolic stability studies, and an in vivo assay with mice harboring adult S. mansoni worms. Of the 46 compounds tested at 33.3 μM, 13 and 14 compounds killed NTS and adult worms, respectively, within 72 h. Nine compounds had 90% inhibitory concentrations (IC90s) of ≤10 μM against adult worms, with selectivity indexes of ≥2.8. Their physicochemical properties and permeation through an artificial membrane indicated good to moderate intestinal absorption. Their metabolic stabilities ranged from low to high. Despite satisfactory in vitro results and in silico predictions, only one compound resulted in a statistically significant worm burden reduction (66%) after administration of a single oral dose of 400 mg/kg of body weight to S. mansoni-infected mice. Worm burden reductions of 0 to 43% were observed for the remaining eight compounds tested. In conclusion, several analogs of the N,N'-diarylurea MMV665852 had high efficacy against S. mansoni in vitro and favorable physicochemical properties for permeation through the intestinal wall. To counteract the low efficacy observed in the mouse model, further investigations should focus on identifying compounds with improved solubility and pharmacokinetic properties.
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