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Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic antagonists are called...
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Updated: May 14, 2026

Solid-phase Synthesis of [4.4] Spirocyclic Oximes
05:15

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Published on: February 6, 2019

Spirocyclic compounds, potent CCR1 antagonists.

Nafizal Hossain1, Svetlana Ivanova, Jonas Bergare

  • 1Department of Medicinal Chemistry, R&I Innovative Medicines, AstraZeneca R&D, Pepparedsleden 1, Mölndal 431 83, Sweden. Nafizal.Hossain@astrazeneca.com

Bioorganic & Medicinal Chemistry Letters
|February 19, 2013
PubMed
Summary
This summary is machine-generated.

Researchers synthesized novel spirocycles, demonstrating potent inhibition of chemokine receptor type 1 (CCR1) and its associated chemotaxis. These findings highlight potential therapeutic applications for CCR1-targeted diseases.

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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
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Last Updated: May 14, 2026

Solid-phase Synthesis of [4.4] Spirocyclic Oximes
05:15

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Published on: February 6, 2019

Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of &#945;-Imino &#947;-Lactones and Alkylidene Pyrazolones
10:17

Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones

Published on: February 7, 2019

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
05:17

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

Area of Science:

  • Medicinal Chemistry
  • Immunology
  • Pharmacology

Background:

  • Chemokine receptor type 1 (CCR1) plays a crucial role in inflammatory and immune responses.
  • Developing selective CCR1 antagonists is a key therapeutic strategy for various diseases.

Purpose of the Study:

  • To synthesize and characterize novel conformationally constrained spirocyclic compounds.
  • To evaluate the in vitro antagonist activity of these compounds against CCR1.
  • To assess their efficacy in inhibiting CCR1-mediated chemotaxis.

Main Methods:

  • Synthesis of spirocyclic compounds (17-23) and (31-36).
  • In vitro evaluation of CCR1 antagonist potency.
  • Functional assay to determine IC50 values for inhibition of CCR1-mediated chemotaxis.

Main Results:

  • Synthesized spirocycles (17-23) and (31-36) were obtained.
  • Compounds exhibited sub-nanomolar potency as CCR1 antagonists.
  • Compounds 22, 23, and 36 potently inhibited CCR1-mediated chemotaxis with IC50 values of 2 nM, 2.6 nM, and 68 nM, respectively.

Conclusions:

  • The novel spirocyclic compounds are potent CCR1 antagonists.
  • These compounds effectively inhibit CCR1-mediated chemotaxis in vitro.
  • The synthesized spirocycles represent promising candidates for further investigation in CCR1-related therapeutic areas.