Evidence map›Paper›PMID 38912512›Full record

ArticleHeliyon2024

Quinolinyl-based multitarget-directed ligands with soluble epoxide hydrolase and fatty acid amide hydrolase inhibitory activities: Synthetic studies and pharmacological evaluations.

Jeannes Angelia, Leah Duong, Faye Yun, Anesa Mesic, Cassandra Yuan, Daniel Carr, Siena Gunari, Paula K Hudson, Christophe Morisseau, Bruce D Hammock and 2 more

Abstract read
In one paragraph

Article in Heliyon, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing 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

5 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  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

12 authors.

Jeannes AngeliaDepartment of Chemistry & Biochemistry, California State University, Fullerton, 800 N. State College, Fullerton, CA, 92834, United States.
Leah DuongDepartment of Chemistry & Biochemistry, California State University, Fullerton, 800 N. State College, Fullerton, CA, 92834, United States.
Faye YunDepartment of Chemistry & Biochemistry, California State University, Fullerton, 800 N. State College, Fullerton, CA, 92834, United States.
Anesa MesicDepartment of Chemistry & Biochemistry, California State University, Fullerton, 800 N. State College, Fullerton, CA, 92834, United States.
Cassandra YuanDepartment of Psychology, California State University, East Bay, 25800 Carlos Bee Blvd. Science S229, Hayward, CA, 94542, United States.
Daniel CarrDepartment of Psychology, California State University, East Bay, 25800 Carlos Bee Blvd. Science S229, Hayward, CA, 94542, United States.
Siena GunariDepartment of Psychology, California State University, East Bay, 25800 Carlos Bee Blvd. Science S229, Hayward, CA, 94542, United States.
Paula K HudsonDepartment of Chemistry & Biochemistry, California State University, Fullerton, 800 N. State College, Fullerton, CA, 92834, United States.
Christophe MorisseauDepartment of Entomology and Nematology, and UCD Comprehensive Cancer Center, University of California Davis, Davis, CA, 95616, United States.
Bruce D HammockDepartment of Entomology and Nematology, and UCD Comprehensive Cancer Center, University of California Davis, Davis, CA, 95616, United States.
Ram KandasamyDepartment of Psychology, California State University, East Bay, 25800 Carlos Bee Blvd. Science S229, Hayward, CA, 94542, United States.
Stevan PecicDepartment of Chemistry & Biochemistry, California State University, Fullerton, 800 N. State College, Fullerton, CA, 92834, United States.

Funding

Supplement for bioactive lipids as effectors and indicators of the deleterious effects of human healthR35ES030443 · NIEHS · UNIVERSITY OF CALIFORNIA AT DAVIS · PI MORISSEAU, CHRISTOPHE HP · 2019 to 2025
$5.8M
U-RISE at Cal State FullertonT34GM149493 · NIGMS · CALIFORNIA STATE UNIVERSITY FULLERTON · PI MATH P CUAJUNGCO · 2023 to 2026
$1.3M
Designed Multiple Ligands as Non-opioid Analgesics for Treating Chronic PainR16GM149204 · NIGMS · CALIFORNIA STATE UNIVERSITY FULLERTON · PI Stevan Pecic · 2023 to 2026
$650k
NIEHS NIH HHS R35 ES030443NIGMS NIH HHS R16 GM149204NIGMS NIH HHS T34 GM149493
6 · The paper itself

Abstract

Simultaneous inhibition of soluble epoxide hydrolase (sEH) and fatty acid amide hydrolase (FAAH) with a single small molecule represents a novel therapeutic approach in treating inflammatory pain, since both targets are involved in pain and inflammation processes. In this study using multi-target directed ligands methodology we designed and synthesized 7 quinolinyl-based dual sEH/FAAH inhibitors, using an optimized microwave-assisted Suzuki-Miyaura coupling reaction and tested their potency in human FAAH and human, rat, and mouse sEH inhibition assays. The structure-activity relationship study showed that quinolinyl moiety is well tolerated in the active sites of both enzymes, yielding several very potent dual sEH/FAAH inhibitors with the IC

Indexed as

Enzyme inhibitionFormalin testMicrowave-assisted synthesisMolecular modelingMulti-target directed ligandsStructure-activity relationship studySuzuki coupling reaction

Identifiers

PMID38912512
PMCPMC11190605

What OpenQuestion 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 OpenQuestion graph.