Evidence map›Paper›PMID 25466924›Full record

ReviewEuropean journal of medicinal chemistry2015

Bioactive heterocycles containing endocyclic N-hydroxy groups.

Reshma Rani, Carlotta Granchi

Abstract readReview
In one paragraph

Review in European journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.6field-weighted citation impact, top 18% of its field
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

11 citing papers in PubMed, 47 citations in OpenAlex.

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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

2 authors at 1 institution in 1 country.

Reshma RaniDipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
Carlotta GranchiDipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy. Electronic address: carlotta.granchi@farm.unipi.it.
University of Pisa · IT

Funding

Design, Synthesis, and Evaluation of Lactate Dehydrogenase InhibitorsR01GM098453 · NIGMS · UNIVERSITY OF ILLINOIS AT URBANA-CHAMPAIGN · PI HERGENROTHER, PAUL · 2012 to 2015
$1.8M
NIGMS NIH HHS R01 GM098453NIGMS NIH HHS R01GM098453
6 · The paper itself

Abstract

Drug-likeness rules consider N-O single bonds as "structural alerts" which should not be present in a perspective drug candidate. In most cases this concern is correct, since it is known that N-hydroxy metabolites of branded drugs produce reactive species that cause serious side effects. However, this dangerous reactivity of the N-OH species generally takes place when the nitrogen atom is not comprised in a cyclic moiety. In fact, the same type of metabolic behavior should not be expected when the nitrogen atom is included in the ring of an aromatic heterocyclic scaffold. Nevertheless, heterocycles bearing endocyclic N-hydroxy portions have so far been poorly studied as chemical classes that may provide new therapeutic agents. This review provides an overview of N-OH-containing heterocycles with reported bioactivities that may be considered as therapeutically relevant and, therefore, may extend the chemical space available for the future development of novel pharmaceuticals. A systematic treatment of the various chemical classes belonging to this particular family of molecules is described along with a discussion of the biological activities associated to the most important examples.

Indexed as

Drug DiscoveryAnimalsDrug DesignHeterocyclic CompoundsHumansHydroxidesMolecular StructureStructure-Activity RelationshipHeterocyclic Compoundshydroxide ionHydroxidesBioactivityMetabolismN-Hydroxy-heterocycles

Identifiers

PMID25466924
PMCPMC4436092
OpenAlexW1983108233

What OpenQuestion holds

Textmetadata
LicenceTDM
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 OpenQuestion graph.