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Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties
- Source :
- European journal of medicinal chemistry. 241
- Publication Year :
- 2022
-
Abstract
- The design of compounds able to combine the selective inhibition of cyclooxygenase-2 (COX-2) with the release of nitric oxide (NO) is a promising strategy to achieve potent anti-inflammatory agents endowed with an overall safer profile and reduced toxicity upon gastrointestinal and cardiovascular systems. With the aim of generating novel and selective COX-2 inhibiting NO-donors (CINOD) and encouraged by the promising results obtained with our nitrooxy- and hydroxyethyl ethers 11 and 12 reported in previous works, we shifted our attention on the synthesis of isosteric thioanalogs nitrooxy- and hydroxy ethyl sulfides 13a-c and 14a-c, respectively, along with their oxidation products nitrooxy- and hydroxyethyl sulfoxides 15a-c and 16a-c, respectively, also referred to as thio-CINOD. Preliminary data and metabolic analysis highlighted how the isosteric substitution of the ethereal oxygen atom of 11a-c with sulfur in compounds 13a-c, independently from the presence and the number of fluorine atoms in N
- Subjects :
- Vasodilator Agents
Anti-Inflammatory Agents
Sulfides
Selective COX-2 inhibitors
Mice
Drug Discovery
Animals
Nitric Oxide Donors
Pyrroles
Antinociceptive agents
Pharmacology
Analgesics
Cyclooxygenase 2 Inhibitors
Organic Chemistry
Anti-Inflammatory Agents, Non-Steroidal
Vasorelaxation
General Medicine
1,5-Diarylpyrrole derivatives
5-Diarylpyrrole derivatives
Oxygen
Cyclooxygenase 2
Sulfoxides
Cyclooxygenase 1
Sulfur
Ethers
Subjects
Details
- ISSN :
- 17683254
- Volume :
- 241
- Database :
- OpenAIRE
- Journal :
- European journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....bfd9ad58bbfe8e7adff66bdb69561884