Evidence map›Paper›PMID 32214795›Full record

ArticleDrug design, development and therapy2020

In silico Design and Synthesis of Tetrahydropyrimidinones and Tetrahydropyrimidinethiones as Potential Thymidylate Kinase Inhibitors Exerting Anti-TB Activity Against

Katharigatta N Venugopala, Christophe Tratrat, Melendhran Pillay, Sandeep Chandrashekharappa, Omar Husham Ahmed Al-Attraqchi, Bandar E Aldhubiab, Mahesh Attimarad, Osama I Alwassil, Anroop B Nair, Nagaraja Sreeharsha and 6 more

Abstract read
In one paragraph

Article in Drug design, development and therapy, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing 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

11 citing papers in PubMed.

  1. Review
  2. Review
  3. Review
  4. Review
  5. Article
  6. The progress ofFrontiers in medicine · 2024
    Review
  7. Article
  8. Article
  9. Article
  10. Article
  11. 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

16 authors.

Katharigatta N VenugopalaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of Saudi Arabia.ORCID 0000-0003-0680-1549
Christophe TratratDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of Saudi Arabia.ORCID 0000-0001-9064-1706
Melendhran PillayDepartment of Microbiology, National Health Laboratory Services, KZN Academic Complex, Inkosi Albert Luthuli Central Hospital, Durban 4001, South Africa.ORCID 0000-0002-5570-1010
Sandeep ChandrashekharappaInstitute for Stem Cell Biology and Regenerative Medicine, NCBS, TIFR, Bangalore 560 065, India.ORCID 0000-0003-2475-7270
Omar Husham Ahmed Al-AttraqchiDepartment of Pharmaceutical Sciences, Faculty of Pharmacy, Philadelphia University, Amman 19392, Jordan.
Bandar E AldhubiabDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of Saudi Arabia.ORCID 0000-0002-2684-4186
Mahesh AttimaradDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of Saudi Arabia.ORCID 0000-0002-7007-9119
Osama I AlwassilDepartment of Pharmaceutical Sciences, College of Pharmacy, King Saud Bin Abdulaziz University for Health Sciences, Riyadh, Saudi Arabia.ORCID 0000-0002-6572-8321
Anroop B NairDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of Saudi Arabia.ORCID 0000-0003-2850-8669
Nagaraja SreeharshaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of Saudi Arabia.ORCID 0000-0002-2058-255X
Rashmi VenugopalaDepartment of Public Health Medicine, University of KwaZulu-Natal, Howard College Campus, Durban 4001, South Africa.ORCID 0000-0002-1101-4577
Mohamed A MorsyDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of Saudi Arabia.ORCID 0000-0002-6752-9094
Michelyne HarounDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of Saudi Arabia.ORCID 0000-0003-1521-1399
Hezekiel M KumaloDepartment of Medical Biochemistry, School of Laboratory Medicine and Medical Sciences, University of KwaZulu-Natal, Medical School, Durban 4001, South Africa.
Bharti OdhavDepartment of Biotechnology and Food Technology, Durban University of Technology, Durban 4001, South Africa.ORCID 0000-0002-2264-5948
Koleka MlisanaDepartment of Microbiology, National Health Laboratory Services, KZN Academic Complex, Inkosi Albert Luthuli Central Hospital, Durban 4001, South Africa.ORCID 0000-0002-8436-3268

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

background and purposeTuberculosis has been reported to be the worldwide leading cause of death resulting from a sole infectious agent. The emergence of multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis has made the battle against the infection more difficult since most currently available therapeutic options are ineffective against these resistant strains. Therefore, novel molecules need to be developed to effectively treat tuberculosis disease. Preliminary docking studies revealed that tetrahydropyrimidinone derivatives have favorable interactions with the thymidylate kinase receptor. In the present investigation, we report the synthesis and the mycobacterial activity of several pyrimidinones and pyrimidinethiones as potential thymidylate kinase inhibitors.

methodsThe title compounds (

resultsOf the compounds tested for anti-TB activity, pyrimidinone

conclusionPyrimidinone

Indexed as

Drug DesignAntitubercular AgentsDose-Response Relationship, DrugEnzyme InhibitorsMicrobial Sensitivity TestsMolecular StructureMycobacterium tuberculosisNucleoside-Phosphate KinasePyrimidinonesStructure-Activity RelationshipAntitubercular AgentsdTMP kinaseEnzyme InhibitorsNucleoside-Phosphate KinasePyrimidinonestetrahydropyrimidinonemolecular modelingmultidrug resistanceMycobacterium tuberculosistetrahydropyrimidinethionestetrahydropyrimidinonesthymidylate kinase inhibitors

Identifiers

PMID32214795
PMCPMC7082623

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.