ArticleBiomolecules2026
Synthesis and Biological Profiling of New 1,2,3,4-Tetrahydrobenzo[
Aldrick B Verano, Anna Sampietro, Ana Mallo-Abreu, Rosaria Spagnuolo, Belén Pérez, Manuela Bartolini, María Isabel Loza, José Brea, Jordi Juárez-Jiménez, Raimon Sabate and 2 more
Abstract read
In one paragraphArticle in Biomolecules, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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5 · Who and what moneyAuthors and funding
12 authors.
Aldrick B VeranoLaboratory of Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII 27-31, E-08028 Barcelona, Spain.ORCID 0000-0003-0958-8421 Anna SampietroLaboratory of Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII 27-31, E-08028 Barcelona, Spain.ORCID 0000-0002-1837-2051 Ana Mallo-AbreuLaboratory of Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII 27-31, E-08028 Barcelona, Spain.ORCID 0000-0002-5092-3538 Rosaria SpagnuoloDepartment of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, I-40126 Bologna, Italy.ORCID 0009-0002-0289-6763 Belén PérezDepartment of Pharmacology, Therapeutics and Toxicology, Autonomous University of Barcelona, E-08193 Bellaterra, Spain.ORCID 0000-0001-5801-1704 Manuela BartoliniDepartment of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, I-40126 Bologna, Italy.ORCID 0000-0002-2890-3856 María Isabel LozaBioFarma Research Group, Centro Singular de Investigación en Medicina Molecular y Enfermedades Crónicas (CIMUS), Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, Universidade de Santiago de Compostela, Av. de Barcelona s/n, E-15782 Santiago de Compostela, Spain.
José BreaBioFarma Research Group, Centro Singular de Investigación en Medicina Molecular y Enfermedades Crónicas (CIMUS), Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, Universidade de Santiago de Compostela, Av. de Barcelona s/n, E-15782 Santiago de Compostela, Spain.ORCID 0000-0002-5523-1979 Jordi Juárez-JiménezDepartment of Pharmacy and Pharmaceutical Technology and Physical-Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII 27-31, E-08028 Barcelona, Spain.
Raimon SabateInstitute of Biomedicine of the University of Barcelona (IBUB), Av. Diagonal 643, E-08028 Barcelona, Spain.ORCID 0000-0003-3894-2362 Carles GaldeanoInstitute of Biomedicine of the University of Barcelona (IBUB), Av. Diagonal 643, E-08028 Barcelona, Spain.ORCID 0000-0003-1702-0369 Diego Muñoz-TorreroLaboratory of Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII 27-31, E-08028 Barcelona, Spain.ORCID 0000-0002-8140-8555 Funding
MICIU/AEI/10.13039/501100011033 PID2023-147004OB-I00
6 · The paper itselfAbstract
DP-128 is a multitarget benzonaphthyridine-6-chlorotacrine hybrid molecule with potent in vitro anticholinesterase and Aβ42 and tau anti-aggregating activity. While often used as a reference protein aggregation inhibitor, its further development as an anti-Alzheimer agent is limited by significant cytotoxicity, suboptimal aqueous solubility and microsomal stability. Since these drawbacks might arise from its rather high lipophilicity, in this work we have developed a series of more polar analogues, designed by structural modifications at the benzonaphthyridine or 6-chlorotacrine moieties or within the eight-atom linker. Half of the new analogues are indeed slightly more soluble and clearly less cytotoxic than DP-128, display single-digit acetylcholinesterase inhibitory activity, and retain the Aβ42 and tau anti-aggregating potency of the lead, as well as favourable brain permeation and high plasma stability. While further optimization of microsomal stability is necessary for a potential therapeutic use of this class of compounds, hybrids
Indexed as
Amyloid beta-PeptidesCholinesterase InhibitorsNaphthyridinestau ProteinsAcetylcholinesteraseAnimalsHumansPeptide FragmentsProtein AggregatesAcetylcholinesteraseAmyloid beta-Peptidesamyloid beta-protein (1-42)Cholinesterase InhibitorsNaphthyridinesPeptide FragmentsProtein Aggregatestau Proteinsacetylcholinesterase inhibitionAlzheimer’s diseaseamyloid aggregation inhibitionDMPK propertiesmultitarget agents
Identifiers
PMID42072714
PMCPMC13113287
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