Cited by 45Cholinesterase and Neurodegenerative DiseasesAlzheimer's disease research and treatmentsSynthesis and biological activity

New Dual Small Molecules for Alzheimer’s Disease Therapy Combining Histamine H 3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition

Open access
Malek, Rim, Arribas, Raquel L., Palomino-Antolin, Alejandra, Totoson, Perle, Demougeot, Celine, Kobrlova, Tereza, Soukup, Ondrej, Iriepa, Isabel +14 more·2019·Journal of Medicinal Chemistry

Abstract

New tritarget small molecules combining Ca 2+ channels blockade, cholinesterase, and H3 receptor inhibition were obtained by multicomponent synthesis. Compound 3p has been identified as a very promising lead, showing good Ca 2+ channels blockade activity (IC 50 = 21 ± 1 μM), potent affinity against hH3R ( K i = 565 ± 62 nM), a moderate but selective hBuChE inhibition (IC 50 = 7.83 ± 0.10 μM), strong antioxidant power (3.6 TE), and ability to restore cognitive impairment induced by lipopolysaccharide.

Integrity signals

Registry

Crossref · 10.1021/acs.jmedchem.9b00937

Cites

48 of 48 references verified0 citation errors · 0 not checkable

Statistics

Recomputing p-values needs the paper’s full text.

Claims the paper makes

We couldn’t retrieve this paper’s full text, so its claims and self-check weren’t run. The registry and citation checks still apply.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

Cites

Flagged first, then by citations

Cited by

Sorted by citations

Authors
Malek, R., Arribas, R. L., Palomino-Antolin, A., Totoson, P., Demougeot, C., Kobrlova, T., Soukup, O., Iriepa, I., Moraleda, I., Diez-Iriepa, D., Godyń, J., Panek, D., Malawska, B., Głuch-Lutwin, M., Mordyl, B., Siwek, A., Chabchoub, F., Marco-Contelles, J., Kiec-Kononowicz, K., Egea, J., de los Ríos, C., & Ismaili, L.
Affiliations
  • University of Sfax (TN)
  • Hospital Universitario de La Princesa (ES)
  • Instituto Teofilo Hernando, Universidad Autónoma de Madrid, C/Arzobispo Morcillo, 4, 28029 Madrid, Spain
  • Université Bourgogne Franche-Comté (FR)
  • EA4267 PEPITE, Université Bourgogne Franche-Comté, F-25030, Besançon, France
  • Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, University of Defence, CZ-500 01 Hradec Kralove, Czech Republic
  • Universidad de Alcalá (ES)
  • Laboratory of Medicinal Chemistry, IQOG, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain
  • Jagiellonian University (PL)
  • Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland
  • Hospital Universitario Santa Cristina (ES)
  • Servicio de Farmacología Clínica, Instituto de Investigación Sanitaria, Hospital Universitario de la Princesa, C/Diego de León, 62, 28006 Madrid, Spain
  • Neurosciences Intégratives et Cliniques EA 481, Pôle de Chimie Organique et Thérapeutique, Université Bourgogne Franche-Comté, UFR Santé, 19, Rue Ambroise Paré, F-25000 Besançon, France
Venue
Journal of Medicinal Chemistry
Published
2019-11-14
Volume
62
Issue
24
Pages
11416-11422
ISSN
  • 0022-2623 (ISSN-L)
  • 1520-4804
OpenAlex
W2990328127
Cited by
45
References
48
Citations by year
2026: 5 · 2025: 5 · 2024: 5 · 2023: 5 · 2022: 7 · 2021: 7 · 2020: 11
FWCI
4.18
Type
journal article
Language
en
Open access
Locations
  • Journal of Medicinal Chemistry (publishedVersion)
  • PubMed (publishedVersion)
  • Jagiellonian University Repository (Jagiellonian University) (submittedVersion, cc-by-nc-nd)
  • HAL (submittedVersion)
Funders
  • Fundaci?n Mutua Madrile?a
  • Uniwersytet Jagiellonski Collegium Medicum (K/ZDS/007121)
  • European Regional Development Fund (CP14/00008, PI16/00735, PI16/01041)
  • European Cooperation in Science and Technology (CA15135)
  • Instituto de Salud Carlos III (CP14/00008, PI16/00735, PI16/01041)
  • Regional Council of Franche-Comt? (04560, 2016YC-04540)
Topics
  • Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
  • Health Sciences › Medicine › Physiology › Alzheimer's disease research and treatments
  • Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
Keywords
Alzheimer's disease, calcium channel blockade, cholinesterase inhibition, multicomponent synthesis, butyrylcholinesterase, antioxidant activity, lead compounds
MeSH terms
Alzheimer Disease, Animals, Calcium Channel Blockers, Cholinesterase Inhibitors, Humans, Memory Disorders, Neuroblastoma, Tumor Cells, Cultured, Vasodilator Agents, Receptors, Histamine H3, Neuroprotective Agents, Mice, Small Molecule Libraries

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review