ArticleACS medicinal chemistry letters2014
Diversity-oriented synthesis yields a new drug lead for treatment of chagas disease.
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 41 citations in OpenAlex.
- Enantioselective Synthesis of Oxazocines via MQ-Phos Enabled Palladium-Catalyzed Asymmetric Formal [4+4]-Cycloadditions.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Automated Solid Phase Assisted Synthesis of a Heparan Sulfate Disaccharide Library.Organic chemistry frontiers : an international journal of organic chemistry · 2022Article
- Re-engineering natural products to engage new biological targets.Natural product reports · 2020Article
- Bridging the gap between natural product synthesis and drug discovery.Natural product reports · 2020Review
- Chemical probes and drug leads from advances in synthetic planning and methodology.Nature reviews. Drug discovery · 2018Review
- High throughput methods to measure the propensity of compounds to form intramolecular hydrogen bonding.MedChemComm · 2017Review
- Novel diversity-oriented synthesis-derived respiratory syncytial virus inhibitors identified via a high throughput replicon-based screen.Antiviral research · 2016Article
- Groebke-Blackburn-Bienaymé multicomponent reaction: emerging chemistry for drug discovery.Molecular diversity · 2016Review
- Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.Cell · 2015Review
- Synthesis of oxazocenones via gold(I)-catalyzed 8-endo-dig hydroalkoxylation of alkynamides.Organic letters · 2015Article
- High throughput screening for anti-Trypanosoma cruzi drug discovery.PLoS neglected tropical diseases · 2014Review
- Drug strategies targeting CYP51 in neglected tropical diseases.Chemical reviews · 2014Review
- Kinases as druggable targets in trypanosomatid protozoan parasites.Chemical reviews · 2014Review
- Impact of stereospecific intramolecular hydrogen bonding on cell permeability and physicochemical properties.Journal of medicinal chemistry · 2014Article
Corrections and comments
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Authors and funding
20 authors at 6 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A phenotypic high-throughput screen using ∼100,000 compounds prepared using Diversity-Oriented Synthesis yielded stereoisomeric compounds with nanomolar growth-inhibition activity against the parasite Trypanosoma cruzi, the etiological agent of Chagas disease. After evaluating stereochemical dependence on solubility, plasma protein binding and microsomal stability, the SSS analogue (5) was chosen for structure-activity relationship studies. The p-phenoxy benzyl group appended to the secondary amine could be replaced with halobenzyl groups without loss in potency. The exocyclic primary alcohol is not needed for activity but the isonicotinamide substructure is required for activity. Most importantly, these compounds are trypanocidal and hence are attractive as drug leads for both acute and chronic stages of Chagas disease. Analogue (5) was nominated as the molecular libraries probe ML341 and is available through the Molecular Libraries Probe Production Centers Network.
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