Evidence map›Paper›PMID 34174633›Full record

ArticleBioorganic chemistry2021

Synthesis, in vitro biological investigation, and molecular dynamics simulations of thiazolopyrimidine based compounds as corticotrophin releasing factor receptor-1 antagonists.

Hossam R Elgiushy, Nageh A Abou-Taleb, George G Holz, Oleg G Chepurny, Ioannis Pirmettis, Sotirios Kakabakos, Vlasios Karageorgos, George Liapakis, Amgad Albohy, Khaled A M Abouzid and 1 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic chemistry, 2021. 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
0.5field-weighted citation impact, top 48% 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

3 citing papers in PubMed, 5 citations in OpenAlex.

  1. Synthesis andRSC advances · 2026
    Article
  2. Endocrinological Treatment Targets for Depressive Disorder.Advances in experimental medicine and biology · 2024
    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

11 authors at 6 institutions in 3 countries.

Hossam R ElgiushyPharmaceutical Chemistry Department, Faculty of Pharmacy, Helwan University, Ain Helwan 11795, Cairo, Egypt; Basic and Applied Sciences Institute, Egypt-Japan University of Science and Technology (E-JUST), New Borg El-Arab City, 21934 Alexandria, Egypt.
Nageh A Abou-TalebPharmaceutical Chemistry Department, Faculty of Pharmacy, Helwan University, Ain Helwan 11795, Cairo, Egypt.
George G HolzDepartment of Medicine, SUNY Upstate Medical University, Syracuse, NY, USA.
Oleg G ChepurnyDepartment of Medicine, SUNY Upstate Medical University, Syracuse, NY, USA.
Ioannis PirmettisInstitute of Nuclear & Radiological Sciences & Technology, Energy & Safety, National Centre for Scientific Research "Demokritos", Athens, Greece.
Sotirios KakabakosInstitute of Nuclear & Radiological Sciences & Technology, Energy & Safety, National Centre for Scientific Research "Demokritos", Athens, Greece.
Vlasios KarageorgosDepartment of Pharmacology, School of Medicine, University of Crete, Voutes, 71003, Heraklion, Crete, Greece.
George LiapakisDepartment of Pharmacology, School of Medicine, University of Crete, Voutes, 71003, Heraklion, Crete, Greece.
Amgad AlbohyDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, The British University in Egypt (BUE), El-Sherouk City, Suez Desert Road, Cairo 11837, Egypt.
Khaled A M AbouzidPharmaceutical Chemistry Department, Faculty of Pharmacy, Ain Shams University, Abbassia 11566, Cairo, Egypt; Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Sadat City, Sadat City, Egypt. Electronic address: khaled.abouzid@pharma.asu.edu.eg.
Sherif F HammadPharmaceutical Chemistry Department, Faculty of Pharmacy, Helwan University, Ain Helwan 11795, Cairo, Egypt; Basic and Applied Sciences Institute, Egypt-Japan University of Science and Technology (E-JUST), New Borg El-Arab City, 21934 Alexandria, Egypt. Electronic address: sherif.hammad@ejust.edu.eg.
SUNY Upstate Medical University · USUniversity of Crete · GRBritish University in Egypt · EGHelwan University · EGInstitute of Nuclear & Radiological Sciences and Technology, Energy & SafetyNational Centre of Scientific Research "Demokritos" · GR

Funding

Molecular Basis of Antidiabetogenic Hormone ActionR01DK069575 · NIDDK · UPSTATE MEDICAL UNIVERSITY · PI HOLZ, GEORGE G · 2007 to 2017
$2.9M
Alpha7 Nicotinic Acetylcholine Receptor Regulation of Glucagon-Like Peptide-1 Incretin Hormone Action.R01DK122332 · NIDDK · UPSTATE MEDICAL UNIVERSITY · PI HOLZ, GEORGE G · 2020 to 2023
$1.6M
NIDDK NIH HHS R01 DK069575NIDDK NIH HHS R01 DK122332
6 · The paper itself

Abstract

Corticotrophin releasing factor receptor-1 (CRFR1) is a potential target for treatment of depression and anxiety through modifying stress response. A series of new thiazolo[4,5-d]pyrimidine derivatives were designed, prepared and biologically evaluated as potential CRFR1 antagonists. Four compounds produced more than fifty percent inhibition in the [

Indexed as

Molecular Dynamics SimulationCRF Receptor, Type 1Dose-Response Relationship, DrugHEK293 CellsHumansMolecular StructurePyrimidinesReceptors, Corticotropin-Releasing HormoneStructure-Activity RelationshipThiazolesCRF Receptor, Type 1PyrimidinesReceptors, Corticotropin-Releasing HormoneThiazolesCRFR1 antagonistsMolecular dynamics simulationScaffold hoppingThiazolo[4,5-d]pyrimidine

Identifiers

PMID34174633
PMCPMC8387444
OpenAlexW3166453378

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.