Evidence map›Paper›PMID 27048943›Full record

ArticleBioorganic & medicinal chemistry letters2016

Synthesis and pharmacological evaluation of mono-arylimidamides as antileishmanial agents.

Xiaohua Zhu, Abdelbasset A Farahat, Meena Mattamana, April Joice, Trupti Pandharkar, Elizabeth Holt, Moloy Banerjee, Jamie L Gragg, Laixing Hu, Arvind Kumar and 4 more

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2016. 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
1.5field-weighted citation impact, top 15% 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

10 citing papers in PubMed, 17 citations in OpenAlex.

  1. Article
  2. Review
  3. Review
  4. Synthesis and Biophysical and Biological Studies ofJournal of medicinal chemistry · 2023
    Article
  5. Article
  6. Escaping ESKAPE resistance:Royal Society open science · 2023
    Article
  7. Article
  8. Article
  9. Review
  10. 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

14 authors at 4 institutions in 3 countries.

Xiaohua ZhuDivision of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
Abdelbasset A FarahatDepartment of Chemistry, Georgia State University, Atlanta, GA 30302, USA; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Meena MattamanaDivision of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
April JoiceDivision of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
Trupti PandharkarDivision of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
Elizabeth HoltDepartment of Chemistry, Georgia State University, Atlanta, GA 30302, USA.
Moloy BanerjeeDepartment of Chemistry, Georgia State University, Atlanta, GA 30302, USA.
Jamie L GraggDepartment of Chemistry, Georgia State University, Atlanta, GA 30302, USA.
Laixing HuDepartment of Chemistry, Georgia State University, Atlanta, GA 30302, USA; Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Arvind KumarDepartment of Chemistry, Georgia State University, Atlanta, GA 30302, USA.
Sihyung YangDepartment of Pharmaceutical Chemistry, School of Pharmacy, University of Kansas, Lawrence, KS 66047, USA.
Michael Zhuo WangDepartment of Pharmaceutical Chemistry, School of Pharmacy, University of Kansas, Lawrence, KS 66047, USA.
David W BoykinDepartment of Chemistry, Georgia State University, Atlanta, GA 30302, USA.
Karl A WerbovetzDivision of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA. Electronic address: werbovetz.1@osu.edu.
Georgia State University · USThe Ohio State University · USUniversity of Kansas · USMansoura University · EG

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Arylimidamide (AIA) compounds containing two pyridylimidamide terminal groups (bis-AIAs) possess outstanding in vitro antileishmanial activity, and the frontrunner bis-AIA DB766 (2,5-bis[2-(2-isopropoxy)-4-(2-pyridylimino)aminophenyl]furan) is active in visceral leishmaniasis models when given orally. Eighteen compounds containing a single pyridylimidamide terminal group (mono-AIAs) were synthesized and evaluated for their antileishmanial potential. Six of these compounds exhibited sub-micromolar potency against both intracellular Leishmania donovani and Leishmania amazonensis amastigotes, and three of these compounds also displayed selectivity indexes of 25 or greater for the parasites compared to a J774 macrophage cell line. When given orally at a dose of 100mg/kg/day for five days, compound 1b (N-(3-isopropoxy-4-(5-phenylfuran-2-yl)phenyl)picolinimidamide methanesulfonate) reduced liver parasitemia by 46% in L. donovani-infected mice. Mono-AIAs are thus a new class of candidate molecules for antileishmanial drug development.

Indexed as

Administration, OralAnimalsAntiprotozoal AgentsChemistry Techniques, SyntheticDrug Evaluation, PreclinicalFuransInhibitory Concentration 50Leishmania donovaniLeishmania mexicanaLeishmaniasis, VisceralMacrophagesMice, Inbred BALB CParasitemiaStructure-Activity RelationshipAntiprotozoal AgentsfuranFuransArylimidamideDB766Drug discoveryLeishmaniasis

Identifiers

PMID27048943
PMCPMC4841789
OpenAlexW2309277975

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.