Evidence map›Paper›PMID 22336245›Full record

ArticleBioorganic & medicinal chemistry2012

Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.

Kwakye Peprah, Xue Y Zhu, Suresh V K Eyunni, Jagan R Etukala, Vincent Setola, Bryan L Roth, Seth Y Ablordeppey

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2012. 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. Article
  2. Article
  3. Benzothiazoles from Condensation ofMolecules (Basel, Switzerland) · 2021
    Review
  4. New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.European journal of medicinal chemistry · 2021
    Article
  5. Article
  6. SYA 013 analogs as moderately selective sigma-2 (σBioorganic & medicinal chemistry · 2019
    Article
  7. Article
  8. Copper-Catalyzed, Ceric Ammonium Nitrate MediatedNew journal of chemistry = Nouveau journal de chimie · 2019
    Article
  9. Article
  10. Article
  11. Article
  12. Article
  13. Further evaluation of the tropane analogs of haloperidol.Bioorganic & medicinal chemistry letters · 2014
    Article
  14. Article
  15. 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

7 authors.

Kwakye PeprahDivision of Basic Pharmaceutical Sciences, Florida A&M University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, FL 32307, USA.
Xue Y Zhu
Suresh V K Eyunni
Jagan R Etukala
Vincent Setola
Bryan L Roth
Seth Y Ablordeppey

Funding

THE PREVENTION OF B(A)P INDUCED CELL TRANSFORMATION BY ORGANOSULFUR COMPOUNDSG12RR003020 · NCRR · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI SACHDEVA, MANDIP SINGH · 1985 to 2011
$29.7M
Targeted Nanocarrier Combination Based Therapy for Lung CancerP20MD006738 · NIMHD · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI SOLIMAN, KARAM F.A. · 2012 to 2016
$5.6M
Development of Novel Agents for CNS-related DiseasesSC1GM088451 · NIGMS · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI ABLORDEPPEY, SETH Y · 2009 to 2012
$1.1M
PHARMACEUTICAL RESEARCH CENTERC06RR012512 · NCRR · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI LEWIS, HENRY · 1997 to 1997
–
NCRR NIH HHS C06 RR012512NCRR NIH HHS C06-RR12512-01NCRR NIH HHS G12 RR003020NIGMS NIH HHS 1SC1GM088451-01NIGMS NIH HHS SC1 GM088451NIMHD NIH HHS P20 MD006738
6 · The paper itself

Abstract

Structure-activity relationship studies on 4-(4-(4-chlorophenyl)-1,4-diazepan-1-yl)-1-(4-fluorophenyl)butan-1-one (SYA 013), a homopiperazine analog of haloperidol has resulted in an understanding of the effect of structural modifications on binding affinity at dopamine and serotonin receptor subtypes. Further exploration, using bioisosteric replacement strategies has led to the identification of several new agents including compounds 7, 8, 11 and 12 which satisfy the initial criteria for further exploration as new antipsychotic agents. In addition, compound 18, a D(3) selective tropanol, has been identified as having the potential for further optimization into a useful drug which may combat neuropsychiatric diseases.

Indexed as

Antipsychotic AgentsAzepinesHaloperidolStructure-Activity Relationship4-(4-(4-chlorophenyl)-1,4-diazepan-1-yl)-1-(4-fluorophenyl)butan-1-oneAntipsychotic AgentsAzepinesHaloperidol

Identifiers

PMID22336245
PMCPMC3356581

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.