title: Synthesis, characterization and pharmacological activity of 4-{[1-substituted aminomethyl-4-arylideneamino-5-sulfanyl-4,5-dihydro-1H-1,2,4-triazol-3-yl]methyl}-2H-1,4-benzothiazin-3(4H)-ones.
abstract: A new series of Schiff and Mannich bases derivatives (6) of 4-[(4-amino-5-sulfanyl-4H-1,2,4-triazol-3-yl)methyl]-2H-1,4-benzothiazin-3(4H)-one (4), derived from (3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)acetic acid (3) were synthesized. The structures of all newly synthesized compounds were elucidated by elemental analysis, IR, (1)H NMR and mass spectral data. Synthesized compounds were evaluated for their anti-inflammatory and analgesic activity. Among the tested compounds, the (3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)acetic acid (3) possess analgesic activity comparable to that of pentazocine; activity decreased on derivatization of the carboxylic acid group. However the anti-inflammatory activity of (3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)acetic acid (3) increased by derivatization of the carboxylic acid group and some of the compounds showed anti-inflammatory activity comparable to that of indomethacin.
authors: Department of Studies in Chemistry, Mangalore University, Mangalagangotri 574 199, India.
authors: J
authors: J
authors: Gowda
authors: A M A
authors: AM
authors: Khader
authors: B
authors: B
authors: Kalluraya
authors: Padma
authors: P
authors: Shree
authors: A R
authors: AR
authors: Shabaraya
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry / Q000379:methods; D051381:Rats; D017208:Rats, Wistar; D013055:Spectrophotometry, Infrared; D013843:Thiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000893:Anti-Inflammatory Agents; D013843:Thiazines