Synthesis and Pharmacological Activities of Novel 3-(Isoxazol-3-yl)-quinazolin-4(3H)-one Derivatives

Abstract

Several new 3‐(isoxazol‐3‐yl)‐quinazolin‐4(3H)‐one derivatives were synthesized and tested for their analgesic and antiinflammatory activities, as well as for their acute toxicity and ulcerogenic effect. A few compounds were as active as phenylbutazone in the writhing and acetic acid peritonitis tests. They had a very low ulcerogenic effect.

Synthesis of 3,4,5-Trisubstituted Isoxazoles through Gold-Catalyzed Cascade Cyclization-Oxidative Alkynylation and Cyclization-Fluorination of 2-Alkynone O-Methyloximes

“…1 is an important scaffold frequently found in many natural products and biologically active compounds such as analgesics, 2 antibiotics, 3 antidepressants, 4 and anticancer agent. 5 It has also been used as a synthetic intermediate, building block and chiral ligand in organic synthesis.…”

Double π–π stacking in 2-[(E)-(3,5-dimethylisoxazol-4-yl)diazenyl]benzoic acid

“…Some uses or properties are anti-inflammatory, analgesic and ulcerogenic (Daidone et al, 1999), antimicrobial and antifungal (Bhatt et al, 1998), inhibition of cyclooxygenase-2 (Talley, 1999;Talley et al, 2000), anticancer activity (Li et al, 2003), selective agonist of dopamine D4 receptors (Rowley et al, 1996) and antagonist of GABA (Frolund et al, 2002). Some uses or properties are anti-inflammatory, analgesic and ulcerogenic (Daidone et al, 1999), antimicrobial and antifungal (Bhatt et al, 1998), inhibition of cyclooxygenase-2 (Talley, 1999;Talley et al, 2000), anticancer activity (Li et al, 2003), selective agonist of dopamine D4 receptors (Rowley et al, 1996) and antagonist of GABA (Frolund et al, 2002).…”

Synthesis and anti-inflammatory activity of 1,4-[bis(3-arylmethane sulfonylvinyl)]benzenes, 1,4-[bis(3-arylmethanesulfonylpyrazolyl and isoxazolyl)]benzenes

“…Pyrazoles display various biological properties such as antimicrobial (Ramalingham et al, 1977), anti-tumor (Taylor et al, 1992), anti-bacterial (Budakoti et al, 2006) and anti-inflammatory (Zitouni et al, 2005). In addition, isoxazoles exhibit diverse range of pharmaceutical activities viz, anti-bacterial (Fathalla et al, 2003), anti-viral (Fathalla et al, 2003), anti-cancer (Lee and Kim, 2002;Lilienkampf et al, 2010), analgesic (Li et al, 2003) and anti-inflammatory (Daidone et al, 1999). Indeed, celecoxib Electronic supplementary material The online version of this article (doi:10.1007/s00044-015-1413-x) contains supplementary material, which is available to authorized users.…”