Evidence map›Paper›PMID 18783951›Full record

ArticleBioorganic & medicinal chemistry letters2008

Structure-activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-D-xylulose 5-phosphate synthase.

Jialin Mao, Hyungjin Eoh, Rong He, Yuehong Wang, Baojie Wan, Scott G Franzblau, Dean C Crick, Alan P Kozikowski

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing 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

15 citing papers in PubMed.

  1. Review
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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

8 authors.

Jialin MaoDrug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, USA.
Hyungjin Eoh
Rong He
Yuehong Wang
Baojie Wan
Scott G Franzblau
Dean C Crick
Alan P Kozikowski

Funding

HTS assays for the methylerythritol-4-phosphate pathwayR01AI097550 · NIAID · COLORADO STATE UNIVERSITY · PI CRICK, DEAN C · 2012 to 2014
$1.1M
NIAID NIH HHS R01 AI097550
6 · The paper itself

Abstract

We report on a target-based approach to identify possible Mycobacterium tuberculosis DXS inhibitors from the structure of a known transketolase inhibitor. A small focused library of analogs was assembled in order to begin elucidating some meaningful structure-activity relationships of 3-(4-chloro-phenyl)-5-benzyl-4H-pyrazolo[1,5-a]pyrimidin-7-one. Ultimately we found that 2-methyl-3-(4-fluorophenyl)-5-(4-methoxy-phenyl)-4H-pyrazolo[1,5-a]pyrimidin-7-one, although still weak, was able to inhibit M. tuberculosis DXS with an IC(50) of 10.6 microM.

Indexed as

Drug DesignAntitubercular AgentsCombinatorial Chemistry TechniquesInhibitory Concentration 50Molecular StructureMycobacterium tuberculosisPyrazolesPyrimidinesStructure-Activity RelationshipTransferases2-methyl-3-(4-fluorophenyl)-5-(4-methoxy-phenyl)-4H-pyrazolo(1,5-a)pyrimidin-7-oneAntitubercular Agentsdeoxyxylulose-5-phosphate synthasePyrazolesPyrimidinesTransferases

Identifiers

PMID18783951
PMCPMC4784473

What OpenQuestion 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 OpenQuestion graph.