Evidence map›Paper›PMID 26183840›Full record

ArticleMolecular diversity2015

Exploring structural requirements for peripherally acting 1,5-diaryl pyrazole-containing cannabinoid 1 receptor antagonists for the treatment of obesity.

Mayank Kumar Sharma, Prashant R Murumkar, Rajani Giridhar, Mange Ram Yadav

Abstract read
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In one paragraph

Article in Molecular diversity, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
2.6field-weighted citation impact, top 11% 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

4 citing papers in PubMed, 17 citations in OpenAlex.

  1. Review
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  3. Toxins · 2019
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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

4 authors at 1 institution in 1 country.

Mayank Kumar SharmaPharmacy Department, Faculty of Technology & Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara, 390 001, India.
Prashant R MurumkarPharmacy Department, Faculty of Technology & Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara, 390 001, India.
Rajani GiridharPharmacy Department, Faculty of Technology & Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara, 390 001, India.
Mange Ram YadavPharmacy Department, Faculty of Technology & Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara, 390 001, India. mryadav11@yahoo.co.in.
Maharaja Sayajirao University of Baroda · IN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Peripherally acting cannabinoid 1 (CB1) receptor antagonists are considered as potential therapeutics for the treatment of obesity with desired efficacy and reduced central nervous system side effects. A dataset of 72 compounds containing the 1,5-diaryl pyrazole basic skeleton having peripheral CB1 receptor antagonistic activity was utilized for three-dimensional quantitative structure-activity relationship studies. Compounds of the series exhibited high variations in the biological activity and chemical structures. Different types of molecular alignments, such as atom-based, data-based, centroid-based and centroid/atom-based were utilized to develop the best CoMFA model. The best CoMFA model was obtained with a database alignment and the same alignment was further used for the development of a CoMSIA model. The best developed CoMFA model had [Formula: see text] with six components, [Formula: see text] while the best developed CoMSIA model had [Formula: see text] with six components, [Formula: see text] and [Formula: see text] The predictive [Formula: see text] values of these two models showed test set predictions of 0.528 and 0.679 for the best CoMFA and CoMSIA models, respectively. Based on a higher [Formula: see text] value, the CoMSIA model was found to be the best one. The prediction accuracy and reliability of the best developed CoMSIA model have been validated using well-established methods. Using the inputs from the best CoMSIA contour maps, several novel highly selective peripherally acting CB1 receptor antagonists have been designed and reported herein.

Indexed as

HumansModels, MolecularMolecular StructureObesityPyrazolesQuantitative Structure-Activity RelationshipReceptor, Cannabinoid, CB1PyrazolesReceptor, Cannabinoid, CB11, 5-Diaryl pyrazole3D-QSARCB1 receptor antagonistsEndocannabinoidsRimonabant

Identifiers

PMID26183840
OpenAlexW1424179073

What OpenQuestion holds

Textmetadata
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.