Evidence mapPaperPMID 36077003Full record

ArticleInternational journal of molecular sciences2022

Design, Synthesis, Molecular Modeling and Anti-Hyperglycemic Evaluation of Quinazoline-Sulfonylurea Hybrids as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) and Sulfonylurea Receptor (SUR) Agonists.

Mohamed Ayman El-Zahabi, Faida H Bamanie, Salah Ghareeb, Heba K Alshaeri, Moudi M Alasmari, Mohamed Moustafa, Zohair Al-Marzooki, Mohamed F Zayed

Abstract read
In one paragraph

Article in International journal of molecular sciences, 2022. 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. Review
  4. Review
  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

8 authors.

Mohamed Ayman El-ZahabiPharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo 11884, Egypt.
Faida H BamanieBiochemistry Department, College of Medicine, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Salah GhareebPharmacology Department, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt.
Heba K AlshaeriPharmaceutical Sciences Department, Fakeeh College for Medical Sciences, Jeddah 21461, Saudi Arabia.ORCID 0000-0003-1960-0092
Moudi M AlasmariCollege of Medicine, King Saud Bin Abdulaziz University for Health Sciences (KSAU-HS), Jeddah 21461, Saudi Arabia.
Mohamed MoustafaMedicinal Chemistry Department, Faculty of Pharmacy, Mansurah University, El Mansurah 35516, Egypt.
Zohair Al-MarzookiBiochemistry Department, College of Medicine, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Mohamed F ZayedPharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo 11884, Egypt.ORCID 0000-0001-8683-5460

Funding

King Abdulaziz University 426 / 049
6 · The paper itself

Abstract

New quinazoline-sulfonylurea hybrids were prepared and examined for their in vivo anti-hyperglycemic activities in STZ-induced hyperglycemic rats using glibenclamide as a reference drug. Compounds VI-6-a, V, IV-4, VI-4-c, IV-6, VI-2-a, IV-1, and IV-2 were more potent than the reference glibenclamide. They induced significant reduction in the blood glucose levels of diabetic rats: 78.2, 73.9, 71.4, 67.3, 62, 60.7, 58.4, and 55.9%, respectively, while the reference glibenclamide had 55.4%. Compounds IV-1, VI-2-a, IV-2, V, and IV-6 showed more prolonged antidiabetic activity than glibenclamide. Moreover, molecular docking and pharmacokinetic studies were performed to examine binding modes of the prepared compounds against peroxisome proliferator-activated receptor gamma (PPARγ). The highest active compounds exhibited good binding affinity with high free energy of binding against PPARγ. In silico absorption, distribution, metabolism, elimination and toxicity (ADMET) studies were performed to investigate pharmacokinetics and safety of the synthesized compounds. They showed considerable human intestinal absorption with low toxicity profile.

Indexed as

Diabetes Mellitus, ExperimentalPPAR gammaAnimalsGlyburideHumansHypoglycemic AgentsMolecular Docking SimulationQuinazolinesRatsSulfonylurea CompoundsSulfonylurea ReceptorsGlyburideHypoglycemic AgentsPPAR gammaQuinazolinesSulfonylurea CompoundsSulfonylurea Receptorsanti-hyperglycemicdesignquinazolinesulfonylureasynthesis

Identifiers

PMID36077003
PMCPMC9455857

What Socratic 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 Socratic graph.