Synthesis and Antinociceptive Activity of (2-Benzazolon-3-yl)propionamide Derivatives

• Published in: Archiv der Pharmazie (Weinheim) Vol. 334; no. 1; pp. 17 - 20
• Main Authors: ?nkol, T., Ito, S., Yildirim, E., Erol, K., Sahin, M. F.
• Format: Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag GmbH 01.01.2001; WILEY‐VCH Verlag GmbH; Wiley; Wiley-VCH
• Subjects: (2-benzothiazolinon-3-yl)propionamide; (2-benzoxazolinon-3-yl)propionamide; 1H-NMR; Amides - pharmacology; Analgesics; Analgesics - chemical synthesis; Analgesics - pharmacology; Animals; antinociceptive activity; Biological and medical sciences; Chemistry; Chemistry, Medicinal; Chemistry, Multidisciplinary; Life Sciences & Biomedicine; Magnetic Resonance Spectroscopy; Male; Medical sciences; Mice; Neuropharmacology; Pain Measurement - drug effects; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Physical Sciences; Science & Technology; Spectrophotometry, Infrared; Thiazoles - chemical synthesis; Thiazoles - pharmacology; H-1-NMR; (2-benzothiazolinon-3-yl)propionamide; (2-benzoxazolinon-3-yl)propionamide; antinociceptive activity; Sulfur nitrogen heterocycle; Benzoxazole derivatives; Nitrogen heterocycle; Rodentia; Organic thiocarbamate; Benzothiazole derivatives; Organic carbamate; Vertebrata; Mammalia; Analgesic; Structure activity relation; Mouse; Animal; Bicyclic compound; Aromatic compound; Piperazine derivatives; Chemical synthesis; Oxygen nitrogen heterocycle
• ISSN: 0365-6233; 1521-4184
• DOI: 10.1002/1521-4184(200101)334:1<17::AID-ARDP17>3.0.CO;2-Z

The syntheses of (2‐benzothiazolinon‐3‐yl)propionamide and (2‐benzoxazolinon‐3‐yl)propionamide derivatives are reported. The structures of these compounds are elucidated by their IR and 1H‐NMR spectral data, as well as by elemental analysis. The compounds were tested for antinociceptive activity by hot plate, tail flick, tail clip, and modified Koster tests. Compounds 6b and 7d were found to be the most promising compounds among the substances investigated.