Sudoxicam and related N-heterocyclic carboxamides of 4-hydroxy-2H-1,2-benzothiazine 1,1-dioxide. Potent nonsteroidal antiinflammatory agents

Abstract

Notesol-induced seizures are shown in Table II. All nitrobenzamides exhibited protection which ranged from 20 to 60%. Nitrobenzamides having 3-methylphenyl and 2-methoxyphenyl substituents (3, 6,10,13) at position 1 of the thiocarbamide moiety in both 3-nitroas well as 4-nitrobenzamides were found to exhibit 60% protection against pentylenetetrazol-induced seizures. It is evident from Table II that all 3-nitrobenzamides elicited low mortalities after 24 hr in

Synthesis and pharmacological evaluation of pyrazolopyrimidopyrimidine derivatives: anti-inflammatory agents with gastroprotective effect in rats

“…The structure–activity relationships (SAR) for these compounds have been extensively explored for optimization of anti-inflammatory activity last three decades, since this class was introduced (Lombardino and Wiseman, 1972; Farré et al , 1986; Berq et al , 1999; Lee et al , 1999). In continual efforts to find potentially safer and more efficacious parent agents through further exploration of SAR of this class, we decided to study the pharmacological profiles of compounds 5a , b , f , g belonging to pyrazolopyrimidopyrimidine family.…”

3-[Hydroxy(3-methoxyphenyl)methylidene]-2-(2-oxo-2-phenylethyl)-3,4-dihydro-2H-1λ6,2-benzothiazine-1,1,4-trione

“…The derivatives of 1,2-benzothiazine exhibit a wide range of biological activities, e.g., anti inflammatory (Lombardino & Wiseman, 1972), analgesic (Gupta et al, 2002), anti cancer (Gupta et al, 1993) and anti bacterial (Zia-ur-Rehman et al, 2006), etc. In continuation of our research on the synthesis of biologically active benzothiazine derivatives (Siddiqui et al, 2007;Ahmad et al, 2010), we herein report the synthesis and crystal structure of the title compound.…”

“…For the biological activity of 1,2-benzothiazine derivatives, see : Lombardino & Wiseman (1972); Gupta et al (1993Gupta et al ( , 2002; Zia-ur-Rehman et al (2006); Ahmad et al (2010). For a related structure, see: Siddiqui et al (2008).…”

LIGAND FREE Pd CATALYZED CYCLIZATION-INFLUENCE OF STERIC HINDRANCE

“…The rapid demand for the synthesis of libraries of these types of medicinal compounds with high throughput activities led us towards the synthesis of sultams. Since the time Braun et al synthesized first benzothiazine, thousands of its derivatives have been synthesized and checked for their biological activities [30][31][32][33] . Initially, the most famous and longtime applied methodology for the synthesis of benzothiazine and thiazepine derivatives involved Gabriel-Colman rearrangement 34 .…”