Evidence map›Paper›PMID 30519257›Full record

ArticleThe journal of venomous animals and toxins including tropical diseases2018

Second-generation pterocarpanquinones: synthesis and antileishmanial activity.

Viviane Dos Santos Faiões, Lívia C R M da Frota, Edézio Ferreira Cunha-Junior, Julio C F Barcellos, Thayssa Da Silva, Chaquip Daher Netto, Silvia Amaral Gonçalves Da-Silva, Alcides J M da Silva, Paulo R R Costa, Eduardo Caio Torres-Santos

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PubMed Full text at PMC Publisher
In one paragraph

Article in The journal of venomous animals and toxins including tropical diseases, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed, 1 pooled it
0.7field-weighted citation impact, top 37% 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

5 citing papers in PubMed, 1 synthesis or guideline pooled it, 11 citations in OpenAlex.

  1. Pooled it
  2. Article
  3. Review
  4. Article
  5. 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

10 authors at 3 institutions in 1 country.

Viviane Dos Santos Faiões1Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, FIOCUZ, Av. Brasil, 4365, Pavilhao Leonidas Deane, sala 405A, Manguinhos, Rio de Janeiro, RJ 21040-900 Brazil.
Lívia C R M da Frota2Instituto de Pesquisa de Produtos naturais, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ Brazil.
Edézio Ferreira Cunha-Junior1Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, FIOCUZ, Av. Brasil, 4365, Pavilhao Leonidas Deane, sala 405A, Manguinhos, Rio de Janeiro, RJ 21040-900 Brazil.
Julio C F Barcellos2Instituto de Pesquisa de Produtos naturais, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ Brazil.
Thayssa Da Silva3Laboratório de Imunofarmacologia Parasitária, Universidade do Estado do Rio de Janeiro, Rio de Janeiro, RJ Brazil.
Chaquip Daher Netto4Laboratório de Química, Universidade Federal do Rio de Janeiro, campus Professor Aloísio Teixeira, Macaé, RJ Brazil.
Silvia Amaral Gonçalves Da-Silva3Laboratório de Imunofarmacologia Parasitária, Universidade do Estado do Rio de Janeiro, Rio de Janeiro, RJ Brazil.
Alcides J M da Silva2Instituto de Pesquisa de Produtos naturais, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ Brazil.
Paulo R R Costa2Instituto de Pesquisa de Produtos naturais, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ Brazil.
Eduardo Caio Torres-Santos1Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, FIOCUZ, Av. Brasil, 4365, Pavilhao Leonidas Deane, sala 405A, Manguinhos, Rio de Janeiro, RJ 21040-900 Brazil.ORCID 0000-0003-2240-4519
Universidade Federal do Rio de Janeiro · BRFundação Oswaldo Cruz · BRUniversidade do Estado do Rio de Janeiro · BR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundDespite the development of new therapies for leishmaniasis, among the 200 countries or territories reporting to the WHO, 87 were identified as endemic for Tegumentary Leishmaniasis and 75 as endemic for Visceral Leishmaniasis. The identification of antileishmanial drug candidates is essential to fill the drug discovery pipeline for leishmaniasis. In the hit molecule LQB-118 selected, the first generation of pterocarpanquinones was effective and safe against experimental visceral and cutaneous leishmaniasis via oral delivery. In this paper, we report the synthesis and antileishmanial activity of the second generation of pterocarpanoquinones.

methodsThe second generation of pterocarpanquinones 2a-f was prepared through a palladium-catalyzed oxyarylation of dihydronaphtalen and chromens with iodolawsone, easily prepared by iodination of lawsone. The spectrum of antileishmanial activity was evaluated in promastigotes and intracellular amastigotes of

resultsIn this work, we answered two pertinent questions about the structure of the first-generation pterocarpanquinones: the configuration and positions of rings B (pyran) and C (furan) and the presence of oxygen in the B ring. When rings B and C are exchanged, we noted an improvement of the activity against promastigotes and amastigotes of

conclusionsThe data presented indicate that the pterocarpanoquinones are promising compounds for the development of new leishmanicidal agents.

Indexed as

Drug discoveryLeishmaniaLeishmaniasisLQ-118Neglected diseasesPhenotypic assayPterocarpanquinone

Identifiers

PMID30519257
PMCPMC6263544
OpenAlexW2902121655

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.