Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Pharmacological Evaluation of Novel Bioisosteres of an Adamantanyl Benzamide P2X7 Receptor Antagonist.

ACS chemical neuroscience - 15 Nov 2017

Wilkinson Shane M, Barron Melissa L, O'Brien-Brown James, Janssen Bieneke, Stokes Leanne, Werry Eryn L, Chishty Mansoor, Skarratt Kristen K, Ong Jennifer A, Hibbs David E, Vugts Danielle J, Fuller Stephen, Windhorst Albert D, Kassiou Michael

Abstract excerpt

Adamantanyl benzamide 1 was identified as a potent P2X7R antagonist but failed to progress further due to poor metabolic stability. We describe the synthesis and SAR of a series of bioisosteres of benzamide 1 to explore improvements in the pharmacological properties of this lead. Initial efforts investigated a series of heteroaromatic bioisosteres, which demonstrated improved physicochemical properties but...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Benzamides
Share to Biotransformation

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Drug Evaluation, Preclinical

Share to Drug Stability

Share to Microsomes, Liver

Share to Molecular Structure

Share to Oxidation-Reduction

Share to Receptors, Purinergic P2X7

Source

Identifiers

PMID: 28841278
DOI: 10.1021/acschemneuro.7b00272

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Pharmacological Evaluation of Novel Bioisosteres of an Adamantanyl Benzamide P2X7 Receptor Antagonist.PMID 28841278Read ↗

Quinoline Quest: Kynurenic Acid Strategies for Next-Generation Therapeutics via Rational Drug DesignSemantic proximity Read ↗

Quinoline Quest: Kynurenic Acid Strategies for Next-Generation Therapeutics via Rational Drug DesignSemantic proximity Read ↗

Enabling Asymmetric Synthesis of ABBV-3748, a Corrector Compound for the Treatment of Cystic Fibrosis.Semantic proximity Read ↗

Acyl guanidine inhibitors of β-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.Semantic proximity Read ↗

In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).Semantic proximity Read ↗

Medicinal chemistry of neuronal voltage-gated sodium channel blockers.Semantic proximity Read ↗

Structural insights into the allosteric inhibition of P2X4 receptorsSemantic proximity Read ↗

Non-oxime inhibitors of B-Raf(V600E) kinase.Semantic proximity Read ↗

Potential state-selective hydrogen bond formation can modulate activation and desensitization of the α7 nicotinic acetylcholine receptor.Semantic proximity Read ↗

Molecular-interaction and signaling profiles of AM3677, a novel covalent agonist selective for the cannabinoid 1 receptor.Semantic proximity Read ↗

Experimental and Theoretical Evaluation of the Ethynyl Moiety as a Halogen Bioisostere.Semantic proximity Read ↗

Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.