ArticleEuropean journal of medicinal chemistry2022
Identification and development of a series of disubstituted piperazines for the treatment of Chagas disease.
Article in European journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 10 citations in OpenAlex.
- Late-Stage Functionalization via Thianthrenation: A Reaction Enabling Rapid Preparation of Drug Beads for Chemical Pulldown.Journal of medicinal chemistry · 2026Article
- Mechanistic Exploration ofPharmaceuticals (Basel, Switzerland) · 2026Article
- Structure-activity relationships of 1,5-dihydro-2RSC medicinal chemistry · 2025Article
- Aminopyridines in the development of drug candidates against protozoan neglected tropical diseases.Future medicinal chemistry · 2024Review
- Short-course combination treatment for experimental chronic Chagas disease.Science translational medicine · 2023Article
- Structure-Guided Design and Synthesis of a Pyridazinone Series ofJournal of medicinal chemistry · 2023Article
Corrections and comments
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Authors and funding
25 authors at 3 institutions in 2 countries.
Funding
Abstract
Approximately 6-7 million people around the world are estimated to be infected with Trypanosoma cruzi, the causative agent of Chagas disease. The current treatments are inadequate and therefore new medical interventions are urgently needed. In this paper we describe the identification of a series of disubstituted piperazines which shows good potency against the target parasite but is hampered by poor metabolic stability. We outline the strategies used to mitigate this issue such as lowering logD, bioisosteric replacements of the metabolically labile piperazine ring and use of plate-based arrays for quick diversity scoping. We discuss the success of these strategies within the context of this series and highlight the challenges faced in phenotypic programs when attempting to improve the pharmacokinetic profile of compounds whilst maintaining potency against the desired target.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.