Evidence map›Paper›PMID 26196520›Full record

ArticlePloS one2015

A One Pot Synthesis of Novel Bioactive Tri-Substitute-Condensed-Imidazopyridines that Targets Snake Venom Phospholipase A2.

Nirvanappa C Anilkumar, Mahalingam S Sundaram, Chakrabhavi Dhananjaya Mohan, Shobith Rangappa, Krishna C Bulusu, Julian E Fuchs, Kesturu S Girish, Andreas Bender, Basappa, Kanchugarakoppal S Rangappa

Abstract read
In one paragraph

Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing 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

10 citing papers in PubMed.

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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

10 authors.

Nirvanappa C AnilkumarLaboratory of Chemical Biology, Department of Chemistry, Bangalore University, Central College campus, Palace Road, Bangalore-560 001, Karnataka, India.
Mahalingam S SundaramDepartment of Studies in Biochemistry, University of Mysore, Mysore-570 006, Karnataka, India.
Chakrabhavi Dhananjaya MohanDepartment of Studies in Chemistry, University of Mysore, Mysore-570 006, Karnataka, India.
Shobith RangappaFrontier Research Center for Post-genome Science and Technology Hokkaido University, Sapporo, 060-0808, Japan.
Krishna C BulusuCentre for Molecular Science Informatics, Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW, Cambridge, United Kingdom.
Julian E FuchsCentre for Molecular Science Informatics, Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW, Cambridge, United Kingdom.
Kesturu S GirishDepartment of Studies in Biochemistry, University of Mysore, Mysore-570 006, Karnataka, India; Department of Studies and Research in Biochemistry, Tumkur University, Tumkur-572 103, Karnataka, India.
Andreas BenderCentre for Molecular Science Informatics, Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW, Cambridge, United Kingdom.
BasappaLaboratory of Chemical Biology, Department of Chemistry, Bangalore University, Central College campus, Palace Road, Bangalore-560 001, Karnataka, India.
Kanchugarakoppal S RangappaDepartment of Studies in Chemistry, University of Mysore, Mysore-570 006, Karnataka, India.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Drugs such as necopidem, saripidem, alpidem, zolpidem, and olprinone contain nitrogen-containing bicyclic, condensed-imidazo[1,2-α]pyridines as bioactive scaffolds. In this work, we report a high-yield one pot synthesis of 1-(2-methyl-8-aryl-substitued-imidazo[1,2-α]pyridin-3-yl)ethan-1-onefor the first-time. Subsequently, we performed in silico mode-of-action analysis and predicted that the synthesized imidazopyridines targets Phospholipase A2 (PLA2). In vitro analysis confirmed the predicted target PLA2 for the novel imidazopyridine derivative1-(2-Methyl-8-naphthalen-1-yl-imidazo [1,2-α]pyridine-3-yl)-ethanone (compound 3f) showing significant inhibitory activity towards snake venom PLA2 with an IC50 value of 14.3 μM. Evidently, the molecular docking analysis suggested that imidazopyridine compound was able to bind to the active site of the PLA2 with strong affinity, whose affinity values are comparable to nimesulide. Furthermore, we estimated the potential for oral bioavailability by Lipinski's Rule of Five. Hence, it is concluded that the compound 3f could be a lead molecule against snake venom PLA2.

Indexed as

DaboiaMolecular Docking SimulationPhospholipase A2 InhibitorsPyridinesAnimalsGroup II Phospholipases A2Viper VenomsGroup II Phospholipases A2Phospholipase A2 InhibitorsPyridinesViper VenomsVRV-PL-VIIIa phospholipase A2, Vipera russelli

Identifiers

PMID26196520
PMCPMC4511007

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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.