Piroxicam sulfonates biology-oriented drug synthesis (BIODS), characterization and anti-nociceptive screening

The present study was designed to synthesize aryl/alkyl sulfonyl substituted derivatives of piroxicam. The structures were elucidated through various spectroscopic procedures like 1 H-NMR, 13 C-NMR, MS, IR, UV and elemental analysis. The synthesized derivatives ( I – VI ) were screened for anti-noci...

Full description

Saved in:
Bibliographic Details
Published inMedicinal chemistry research Vol. 25; no. 7; pp. 1468 - 1475
Main Authors Ullah, Safi, Saeed, Muhammad, Halimi, Syed Muhammad Ashhad, Fakhri, Muhammad Imran, Khan, Khalid Mohammed, Khan, Ikhtiar, Perveen, Shahnaz
Format Journal Article
LanguageEnglish
Published New York Springer US 01.07.2016
Subjects
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Original Research
Pharmacology/Toxicology
Piroxicam
Cyclooxygenase
Acetic acid
Analgesic effect
Sulfonyl derivatives
Online AccessGet full text

Cover

More Information
Summary:The present study was designed to synthesize aryl/alkyl sulfonyl substituted derivatives of piroxicam. The structures were elucidated through various spectroscopic procedures like 1 H-NMR, 13 C-NMR, MS, IR, UV and elemental analysis. The synthesized derivatives ( I – VI ) were screened for anti-nociceptive activity in BALB-c mice by dividing them in five groups ( n  = 6) for each compound. Test compounds significantly reduced the number of writhes in acetic acid test for peripheral analgesia, but no effect was observed in hot plate test for central analgesia. The compounds possessed good peripheral analgesic effect but no central effect. These compounds were also assessed for acute toxicity in different doses at 50, 100 and 150 mg/kg i.p., and no mortality was observed in animals. In conclusion, the piroxicam derivatives exhibited marked peripheral anti-nociceptive effect with considerable safety.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-016-1571-5