1-Benzylindoles as inhibitors of cytosolic phospholipase A<sub>2</sub>α: synthesis, biological activity, aqueous solubility, and cell permeability-Reference-Cited by-同舟云学术

1-Benzylindoles as inhibitors of cytosolic phospholipase A₂α: synthesis, biological activity, aqueous solubility, and cell permeability

Published:2024 Issue: Volume: Page:
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Meyer zu Vilsendorf Imke¹,Einerhand Judith¹,Mulac Dennis²,Langer Klaus²,Lehr Matthias¹^ORCID

Affiliation:

1. Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, Corrensstrasse 48, 48149 Münster, Germany

2. Institute of Pharmaceutical Technology and Biopharmacy, University of Münster, Corrensstrasse 48, 48149 Münster, Germany

Abstract

Systematic structural variation of the cytosolic phospholipase A2α (cPLA2α) inhibitor 7, recently found in a ligand-based virtual screening approach, led to the 1-benzylindole derivative 122, which was about 300 times more potent than 7.

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2024/MD/D3MD00590A

Reference26 articles.

1. Pharmacological Control of Phospholipase A2 Activity In Vitro and In Vivo

2. Role of cytosolic phospholipase A2 in allergic response and parturition

3. Reduced fertility and postischaemic brain injury in mice deficient in cytosolic phospholipase A2

4. Structure, function and regulation of Ca2+-sensitive cytosolic phospholipase A2 (cPLA2)

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