Theodoropoulou, Maria A; Psarra, Anastasia; Erhardt, Martin; Nikolaou, Aikaterini; Gerogiannopoulou, Anna-Dimitra D; Hadjipavlou-Litina, Dimitra; Hayashi, Daiki; Dennis, Edward A; Huwiler, Andrea; Kokotos, George (2022). N-Acylated and N-Alkylated 2-Aminobenzothiazoles Are Novel Agents That Suppress the Generation of Prostaglandin E2. Biomolecules, 12(2) MDPI 10.3390/biom12020267
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The quest for novel agents to regulate the generation of prostaglandin E2 (PGE2) is of high importance because this eicosanoid is a key player in inflammatory diseases. We synthesized a series of N-acylated and N-alkylated 2-aminobenzothiazoles and related heterocycles (benzoxazoles and benzimidazoles) and evaluated their ability to suppress the cytokine-stimulated generation of PGE2 in rat mesangial cells. 2-Aminobenzothiazoles, either acylated by the 3-(naphthalen-2-yl)propanoyl moiety (GK510) or N-alkylated by a chain carrying a naphthalene (GK543) or a phenyl moiety (GK562) at a distance of three carbon atoms, stand out in inhibiting PGE2 generation, with EC50 values ranging from 118 nM to 177 nM. Both GK510 and GK543 exhibit in vivo anti-inflammatory activity greater than that of indomethacin. Thus, N-acylated or N-alkylated 2-aminobenzothiazoles are novel leads for the regulation of PGE2 formation.
Item Type: |
Journal Article (Original Article) |
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Division/Institute: |
04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Pharmacology |
UniBE Contributor: |
Erhardt, Martin, Huwiler, Andrea |
Subjects: |
600 Technology > 610 Medicine & health |
ISSN: |
2218-273X |
Publisher: |
MDPI |
Language: |
English |
Submitter: |
Pubmed Import |
Date Deposited: |
01 Mar 2022 14:10 |
Last Modified: |
05 Dec 2022 16:11 |
Publisher DOI: |
10.3390/biom12020267 |
PubMed ID: |
35204768 |
Uncontrolled Keywords: |
N-acylated 2-aminobenzothiazoles N-alkylated 2-aminobenzothiazoles anti-inflammatory agents mesangial cells prostaglandin E2 |
BORIS DOI: |
10.48350/166108 |
URI: |
https://boris.unibe.ch/id/eprint/166108 |
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