ArticleJournal of medicinal chemistry2017
Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis.
Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed.
- Probing Combined Experimental and Computational Profiling to IdentifyMolecules (Basel, Switzerland) · 2026Article
- Imidazo[1,2‑ACS omega · 2026Review
- Extending Thioflavin T Fluorescence Probe to 2-Ethenyl-benzothiazole Derivatives: Drug-like Quadruplex Ligands with Potent Antitrypanosomatid Activity.ACS infectious diseases · 2025Article
- Palladium-catalyzed regioselective C1-selective nitration of carbazoles.Beilstein journal of organic chemistry · 2025Article
- Origami with small molecules: exploiting the C-F bond as a conformational tool.Beilstein journal of organic chemistry · 2025Review
- Multitarget Pharmacology of Sulfur-Nitrogen Heterocycles: Anticancer and Antioxidant Perspectives.Antioxidants (Basel, Switzerland) · 2024Review
- Tinker, Tailor, Soldier, Spy: The Diverse Roles That Fluorine Can Play within Amino Acid Side Chains.Molecules (Basel, Switzerland) · 2023Review
- Optimization of Orally Bioavailable Antileishmanial 2,4,5-Trisubstituted Benzamides.Journal of medicinal chemistry · 2023Article
- Metal-Free Synthesis of Functionalized Quinolines from 2-Styrylanilines and 2-Methylbenzothiazoles/2-Methylquinolines.ACS omega · 2023Article
- Synthetic Approaches to Biologically Active C-2-Substituted Benzothiazoles.Molecules (Basel, Switzerland) · 2022Review
- Current advances in the synthetic strategies of 2-arylbenzothiazole.Molecular diversity · 2022Review
- Synthesis, antiproliferative and antitrypanosomal activities, and DNA binding of novel 6-amidino-2-arylbenzothiazoles.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Development of Novel Isoindolone-Based Compounds against Trypanosoma brucei rhodesiense.ChemistryOpen · 2021Article
- Early Stages of Drug Discovery in an Academic Institution and Involvement of Pharma for Advancing Promising Leads.ACS infectious diseases · 2021Article
- SelectiveACS omega · 2021Article
- Synthesis and Structure-Activity Relationships of Imidazopyridine/Pyrimidine- and Furopyridine-Based Anti-infective Agents against Trypanosomiases.ChemMedChem · 2021Article
- Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.Journal of medicinal chemistry · 2020Review
- Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry.Journal of medicinal chemistry · 2020Article
- Saturated Five-Membered Thiazolidines and Their Derivatives: From Synthesis to Biological Applications.Topics in current chemistry (Cham) · 2020Review
- Phenotypic Drug Discovery for Human African Trypanosomiasis: A Powerful Approach.Tropical medicine and infectious disease · 2020Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
A previous publication from this lab (Patrick, et al. Bioorg. Med. Chem. 2016, 24 , 2451 - 2465 ) explored the antitrypanosomal activities of novel derivatives of 2-(2-benzamido)ethyl-4-phenylthiazole (1), which had been identified as a hit against Trypanosoma brucei, the causative agent of human African trypanosomiasis. While a number of these compounds, particularly the urea analogues, were quite potent, these molecules as a whole exhibited poor metabolic stability. The present work describes the synthesis of 65 new analogues arising from medicinal chemistry optimization at different sites on the molecule. The most promising compounds were the urea derivatives of 2-aryl-benzothiazol-5-amines. One such analogue, (S)-2-(3,4-difluorophenyl)-5-(3-fluoro-N-pyrrolidylamido)benzothiazole (57) was chosen for in vivo efficacy studies based upon in vitro activity, metabolic stability, and brain penetration. This compound attained 5/5 cures in murine models of both early and late stage human African trypanosomiasis, representing a new lead for the development of drugs to combat this neglected disease.
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Registered trials
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