Regioselective alkylation of 1,3,4,5-tetrahydrobenzo[d]azepin-2-one and biological evaluation of the resulting alkylated products as potentially selective 5-HT₂c agonists.

Navnit Prajapati, Rajani Giridhar, Anshuman Sinha, Ashish M Kanhed, Mange Ram Yadav

Abstract read

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. Not yet cited in PubMed.

0numbers the graph read from it

0cells of the map it votes in

0citing papers in PubMed

0.2field-weighted citation impact, top 41% 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

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0 citing papers in PubMed, 2 citations in OpenAlex.

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4 · The record

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5 · Who and what money

Authors and funding

5 authors at 1 institution in 1 country.

Navnit PrajapatiFaculty of Technology & Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara, 390001, Gujarat, India.

Rajani GiridharFaculty of Technology & Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara, 390001, Gujarat, India.

Anshuman SinhaFaculty of Technology & Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara, 390001, Gujarat, India.

Ashish M KanhedFaculty of Technology & Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara, 390001, Gujarat, India.

Mange Ram YadavFaculty of Technology & Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara, 390001, Gujarat, 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

The benzazepine ring system has offered interesting CNS-active medicinal agents. Taking this privileged structure as the basic scaffold, [Formula: see text] and/or [Formula: see text]-alkylated benzazepin-2-one derivatives and their reduced analogs have been prepared as potential [Formula: see text] receptor agonists. The selective alkylation at the [Formula: see text] and/or [Formula: see text] positions of this seven-membered lactam ring is here reported for the first time under different reaction conditions. The synthesized compounds were evaluated for their biological profile as potential [Formula: see text] agonists using a classic pharmacological approach. Three derivatives (15, 17, and 20) have shown promising [Formula: see text] agonistic activity which can be further optimized as anti-obesity agents for the treatment of male sexual dysfunction. Further, a homology model for [Formula: see text] receptor was generated using MODELLER, and ligand-receptor interactions for these potential molecules were studied.

Indexed as

AnimalsBenzazepinesMaleModels, MolecularMolecular StructurePenile ErectionPenisRatsRats, Sprague-DawleySerotonin AntagonistsStructural Homology, ProteinBenzazepinesSerotonin Antagonists3-BenzazepineAnti-obesity agentsPhenethyl fragmentRegioselective alkylationSelective agonists

Identifiers

PMID25916735

DOI10.1007/s11030-015-9600-8

OpenAlexW2091829172

What Socratic 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 Socratic graph.