Evidence map›Paper›PMID 40117080›Full record

ReviewTopics in current chemistry (Cham)2025

Applications of Bridgehead Heterocycles in Drug Design and Medicinal Chemistry.

Simona Di Martino, Pietro Amico, Maria De Rosa

Abstract readReview
PubMed Publisher
In one paragraph

Review in Topics in current chemistry (Cham), 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Heterocycles in Medicinal Chemistry III.Molecules (Basel, Switzerland) · 2026
    Article
  2. 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

3 authors.

Simona Di MartinoMedicinal Chemistry Group, Fondazione Ri.MED, via Filippo Marini 14, 90128, Palermo, Italy.ORCID http://orcid.org/0000-0001-5817-751X
Pietro AmicoMedicinal Chemistry Group, Fondazione Ri.MED, via Filippo Marini 14, 90128, Palermo, Italy.ORCID http://orcid.org/0000-0001-7288-2194
Maria De RosaMedicinal Chemistry Group, Fondazione Ri.MED, via Filippo Marini 14, 90128, Palermo, Italy. mderosa@fondazionerimed.com.ORCID http://orcid.org/0000-0002-4087-2554

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Bridged heterocycles are highly relevant in medicinal chemistry and drug discovery due to the unique features associated with their three-dimensional configuration that ensures great scaffold complexity. In general, inserting bridged systems into a chemical structure positively influences the pharmacokinetic (PK) profile of leads, reducing lipophilicity and enhancing metabolic stability. Several optimization studies show that bridged systems often promoted a significant improvement of the small molecule-enzyme binding interaction due to conformational changes within the biological target active site. To date, many drugs including bridged cores are available in the market to cure several diseases. Given the broad range of biological activities of naturally occurring and (semi)-synthetic bridgehead heterocycles, here, we have thoroughly reviewed the rational design and the structure-activity relationship (SAR) studies of the most remarkable bridged compounds developed during the past decade, to highlight both the chemical and biological roles of these motifs.

Indexed as

Chemistry, PharmaceuticalDrug DesignHeterocyclic CompoundsHumansMolecular StructureStructure-Activity RelationshipHeterocyclic CompoundsBioisosterismBridged systemRigidificationStructure optimizationThree-dimensional

Identifiers

What OpenQuestion holds

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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 OpenQuestion graph.