Synthesis and anti-inflammatory activity of 1-acetyl-5-substitute daryl-3-(β-aminonaphthyl)-2-pyrazolines and β-(substitute daminoethyl) amidonaphthalenes

• Published in: European journal of medicinal chemistry Vol. 36; no. 1; pp. 81 - 92
• Main Authors: Bansal, Ekta, Srivastava, V.K, Kumar, Ashok
• Format: Journal Article
• Language: English
• Published: PARIS CEDEX 15 Elsevier Masson SAS 2001; Elsevier
• Subjects: acute toxicity; anti-inflammatory activity; Biological and medical sciences; Bones, joints and connective tissue. Antiinflammatory agents; chalcones; Chemistry, Medicinal; Life Sciences & Biomedicine; Medical sciences; Pharmacology & Pharmacy; Pharmacology. Drug treatments; pyrazolines; Science & Technology; substituted amidonaphthalene; ulcerogenic activity; chalcones; substituted amidonaphthalene; ulcerogenic activity; acute toxicity; pyrazolines; anti-inflammatory activity; DERIVATIVES; Arene; Rat; Nitrogen heterocycle; Toxicity; Acute; Rodentia; Antiinflammatory agent; Oral administration; Condensed benzenic compound; Naphthalene derivatives; Vertebrata; Gastroduodenal; Mammalia; Structure activity relation; Mouse; Animal; Vinylic compound; Carboxamide; Ulcer; Aromatic compound; Chemical synthesis
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/S0223-5234(00)01179-X

The title compounds were prepared by reaction of β-acetylamino-naphthalene with different aromatic aldehydes followed by cyclisation with hydrazine hydrate and with different primary or secondary amines (Mannich's reaction), respectively. The structures of new compounds were confirmed by 1H-NMR and IR spectral data. Anti-inflammatory and ulcerogenic activities in vivo were evaluated and compared with the standard drugs, phenylbutazone and indomethacin. Some compounds of the series exhibited promising anti-inflammatory activity with a lower ulcerogenic liability than the standard drugs. dkflsdhgkfdjz