Evidence map›Paper›PMID 40128864›Full record

ArticleArchiv der Pharmazie2025

Biginelli dihydropyrimidines and their acetylated derivatives as L-/T-type calcium channel blockers: Synthesis, enantioseparation, and molecular modeling studies.

Miyase Gözde Gündüz, Cagatay Dengiz, Katrin Denzinger, Sun Huang, J T Lee, Jordan W Nafie, Daniel W Armstrong, Gerhard Wolber, Gerald W Zamponi

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Archiv der Pharmazie, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors.

Miyase Gözde GündüzDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Sıhhiye, Ankara, Turkey.ORCID http://orcid.org/0000-0002-2287-9509
Cagatay DengizDepartment of Chemistry, Middle East Technical University, Ankara, Turkey.
Katrin DenzingerMolecular Design Group, Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Freie Universität Berlin, Berlin, Germany.
Sun HuangDepartment of Clinical Neurosciences, Hotchkiss Brain Institute and Alberta Children's Hospital Research Institute, University of Calgary, Calgary, Canada.
J T LeeAZYP, LLC, Arlington, Texas, USA.
Jordan W NafieBioTools Inc., Jupiter, Florida, USA.
Daniel W ArmstrongDepartment of Chemistry & Biochemistry, University of Texas at Arlington, Arlington, Texas, USA.
Gerhard WolberMolecular Design Group, Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Freie Universität Berlin, Berlin, Germany.ORCID http://orcid.org/0000-0002-5344-0048
Gerald W ZamponiDepartment of Clinical Neurosciences, Hotchkiss Brain Institute and Alberta Children's Hospital Research Institute, University of Calgary, Calgary, Canada.

Funding

Hacettepe University Scientific Research Projects Coordination Unit (THD-2020-18712).
6 · The paper itself

Abstract

Biginelli dihydropyrimidines (DHPMs) are considered superior over 1,4-dihydropyridines (DHPs) in terms of both light and metabolic stabilities. Nevertheless, DHPs dominate the market as the most prescribed calcium channel blockers with strong therapeutic potential in managing cardiovascular ailments. To overcome the restrictions that complicate the formulation and postadministration of DHPs, employing bioisosteric replacement by exchanging the DHP ring with DHPM appears as a logical approach for the improved formulations of new calcium channel blockers. In this study, we obtained DHPM derivatives via Biginelli synthesis and acetylated their N-3 position by heating them in acetic anhydride (GD1-GD12). We also incorporated the DHPM scaffold into a condensed ring system (GD13 and GD14). These DHPMs were evaluated for their ability to block both L- (Ca

Indexed as

Calcium Channel BlockersCalcium Channels, L-TypeCalcium Channels, T-TypeDihydropyridinesPyrimidinesAcetylationHumansModels, MolecularMolecular StructureStereoisomerismStructure-Activity RelationshipCalcium Channel BlockersCalcium Channels, L-TypeCalcium Channels, T-TypeDihydropyridinesPyrimidinesBiginelli synthesischiral centermolecular dockingmolecular dynamicspatch clamp

Identifiers

PMID40128864
PMCPMC11933517

What Socratic holds

Textmetadata
LicenceCC BY-NC
Read underepoch 390

Registered trials

None linked

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 Socratic graph.