ArticleJournal of medicinal chemistry2021
Aminoalkoxycarbonyloxymethyl Ether Prodrugs with a pH-Triggered Release Mechanism: A Case Study Improving the Solubility, Bioavailability, and Efficacy of Antimalarial 4(1
Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Evaluation of toll-like receptor inhibition by novel thymoquinone analogues as potential remedy for diabetic nephropathy.Molecular diversity · 2026Article
- Optimization of diastereomeric dihydropyridines as antimalarials.European journal of medicinal chemistry · 2024Article
- Incorporation of an Isohexide Subunit into the Endochin-like Quinolone Scaffold.Molecules (Basel, Switzerland) · 2024Article
- In Vitro Antimalarial Activity of Trichothecenes against Liver and Blood Stages ofJournal of natural products · 2024Article
- Antimalarial Dibenzannulated Medium-Ring Keto Lactams.ACS infectious diseases · 2023Article
- Novel Perspectives on the Design and Development of a Long-Acting Subcutaneous Raltegravir Injection for Treatment of HIV-In Vitro and In Vivo Evaluation.Pharmaceutics · 2023Article
- 7-ACS infectious diseases · 2023Article
- Design, Development, and Optimisation of Smart Linker Chemistry for Targeted Colonic Delivery-In Vitro Evaluation.Pharmaceutics · 2023Article
Corrections and comments
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Authors and funding
15 authors.
Funding
Abstract
Preclinical and clinical development of numerous small molecules is prevented by their poor aqueous solubility, limited absorption, and oral bioavailability. Herein, we disclose a general prodrug approach that converts promising lead compounds into aminoalkoxycarbonyloxymethyl (amino AOCOM) ether-substituted analogues that display significantly improved aqueous solubility and enhanced oral bioavailability, restoring key requirements typical for drug candidate profiles. The prodrug is completely independent of biotransformations and animal-independent because it becomes an active compound via a pH-triggered intramolecular cyclization-elimination reaction. As a proof-of-concept, the utility of this novel amino AOCOM ether prodrug approach was demonstrated on an antimalarial compound series representing a variety of antimalarial 4(1
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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.