7-Chloro-4-phenylsulfonyl quinoline, a new antinociceptive and anti-inflammatory molecule: Structural improvement of a quinoline derivate with pharmacological activity

• Published in: Regulatory toxicology and pharmacology Vol. 90; pp. 72 - 77
• Main Authors: Pinz, Mikaela P., Reis, Angélica S., de Oliveira, Renata Leivas, Voss, Guilherme T., Vogt, Ane G., Sacramento, Manoela do, Roehrs, Juliano A., Alves, Diego, Luchese, Cristiane, Wilhelm, Ethel A.
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier Inc 01.11.2017
• Subjects: Acetic Acid - toxicity; Analgesics - chemistry; Analgesics - pharmacology; Analgesics - therapeutic use; Animals; Anti-Inflammatory Agents - chemistry; Anti-Inflammatory Agents - pharmacology; Anti-Inflammatory Agents - therapeutic use; Croton Oil - toxicity; Edema - chemically induced; Edema - drug therapy; Hot Temperature - adverse effects; Humans; Inflammation; Male; Mice; Nociception; Nociception - drug effects; Pain - drug therapy; Pain - etiology; Quinoline; Quinolines - chemistry; Quinolines - pharmacology; Quinolines - therapeutic use; Stomach Ulcer - chemically induced; Sulfone; Thiazines - pharmacology; Thiazoles - pharmacology; Nociception; Quinoline; Inflammation; Mice; Sulfone
• ISSN: 0273-2300; 1096-0295
• DOI: 10.1016/j.yrtph.2017.08.014

The present study was designed to examine the antinociceptive and anti-inflammatory effects of 7-chloro-4-phenylsulfonyl quinoline (PSOQ). Mice were orally (p.o) pretreated with PSOQ (0.01–10 mg/kg), meloxicam (10 mg/kg), 30 min prior to the acetic acid, hot-plate and open field tests. PSOQ reduced abdominal writhing induced by acetic acid, while meloxicam presented no effect. The latency time in the hot-plate test and locomotor/exploratory activities in the open field test were not altered by treatments. In order to evaluate the gastric tolerability after oral administration of PSOQ or meloxicam (10 mg/kg), mice were fasted for 18 h prior to drug exposure. Four hours later, the development of lesions was assessed. PSOQ and meloxicam did not induce ulcer at the dose and time evaluated. Indeed, anti-inflammatory and anti-edematogenic properties of PSOQ were investigated. For this, animals were pretreated with PSOQ (0.01–50 mg/kg; p.o.), meloxicam (50 mg/kg; p.o.), 30 min prior to croton oil application. PSOQ and meloxicam (50 mg/kg) diminished the edema formation and myeloperoxidase activity induced by croton oil in the ear tissue. Taken together these data demonstrated that PSOQ exerts acute anti-inflammatory and antinociceptive actions, suggesting that it may represent an alternative in the development of future new therapeutic strategies. •PSOQ exerts antinociceptive and anti-inflammatory effects.•PSOQ did not cause gastrointestinal ulceration and sedative effects.•PSOQ suppressed the severity of croton oil via inhibition of MPO activity.