Evidence map›Paper›PMID 27601885›Full record

ArticleDrug design, development and therapy2016

Design, synthesis, and characterization of (1-(4-aryl)- 1H-1,2,3-triazol-4-yl)methyl, substituted phenyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates against Mycobacterium tuberculosis.

Katharigatta N Venugopala, G B Dharma Rao, Subhrajyoti Bhandary, Melendhran Pillay, Deepak Chopra, Bandar E Aldhubiab, Mahesh Attimarad, Osama Ibrahim Alwassil, Sree Harsha, Koleka Mlisana

Abstract read
In one paragraph

Article in Drug design, development and therapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing 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

14 citing papers in PubMed.

  1. Targeting Breast Cancer: Novel Dihydropyrimidinones As Potent Eg5 Inhibitors.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025
    Article
  2. Article
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  5. Journal of enzyme inhibition and medicinal chemistry · 2021
    Article
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  14. Crystal structure analysis of [5-(4-meth-oxy-phen-yl)-2-methyl-2Acta crystallographica. Section E, Crystallographic communications · 2018
    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.

Katharigatta N VenugopalaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Kingdom of Saudi Arabia; Department of Biotechnology and Food Technology, Durban University of Technology, Durban, South Africa.
G B Dharma RaoDepartment of Chemistry, Indian Institute of Science Education and Research Bhopal, Bhopal, India.
Subhrajyoti BhandaryDepartment of Chemistry, Indian Institute of Science Education and Research Bhopal, Bhopal, India.
Melendhran PillayDepartment of Microbiology, National Health Laboratory Services, KZN Academic Complex, Inkosi Albert Luthuli Central Hospital, Durban, South Africa.
Deepak ChopraDepartment of Chemistry, Indian Institute of Science Education and Research Bhopal, Bhopal, India.
Bandar E AldhubiabDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Kingdom of Saudi Arabia.
Mahesh AttimaradDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Kingdom of Saudi Arabia.
Osama Ibrahim AlwassilDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Kingdom of Saudi Arabia.
Sree HarshaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Kingdom of Saudi Arabia.
Koleka MlisanaDepartment of Microbiology, National Health Laboratory Services, KZN Academic Complex, Inkosi Albert Luthuli Central Hospital, Durban, South Africa.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The novel (1-(4-aryl)-1H-1,2,3-triazol-4-yl)methyl, substituted phenyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives were synthesized by the click reaction of the dihydropyrimidinones, bearing a terminal alkynyl group, with various substituted aryl azides at room temperature using a catalytic amount of Cu(OAc)2 and sodium ascorbate in a 1:2 ratio of acetone and water as a solvent. The newly synthesized compounds were characterized by a number of spectroscopic techniques, such as infrared, liquid chromatography-mass spectrometry, (1)H, and (13)C nuclear magnetic resonance along with single crystal X-ray diffraction. The current procedure for the synthesis of 1,2,3-triazole hybrids with dihydropyrimidinones is appropriate for the synthesis of a library of analogs 7a-l and the method accessible here is operationally simple and has excellent yields. The title compounds 7a-l were evaluated for their in vitro antitubercular activity against H37RV and multidrug-resistant strains of Mycobacterium tuberculosis by resazurin microplate assay plate method and it was found that compound 7d was promising against H37RV and multidrug-resistant strains of M. tuberculosis at 10 and 15 μg/mL, respectively.

Indexed as

Drug DesignAntitubercular AgentsDose-Response Relationship, DrugMicrobial Sensitivity TestsMolecular StructureMycobacterium tuberculosisPyrimidinonesStructure-Activity RelationshipTriazoles(1-(4-(trifluoromethyl)phenyl)-1H-1,2,3-triazol-4-yl)methyl 6-methyl-2-oxo-4-(4-(trifluoromethyl)phenyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylateAntitubercular AgentsPyrimidinonesTriazoles123-triazoleantitubercular drug discoveryclick chemistrydihydropyrimidinonesynthesis

Identifiers

PMID27601885
PMCPMC5003518

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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.