[Show abstract][Hide abstract] ABSTRACT: Dual cyclooxygenase/lipoxygenase (COX/LOX) inhibitors constitute a valuable alternative to classical nonsteroidal anti-inflammatory drugs (NSAIDs) and selective COX-2 inhibitors for the treatment of inflammatory diseases. A series of 3-(5-phenyl/phenylamino-[1,3,4]oxadiazol-2-yl)-chromen-2-one and N-[5-(2-oxo-2H-chromen-3-yl)-[1,3,4]oxadiazol-2-yl]-benzamide derivatives were synthesized and screened for anti-inflammatory, analgesic activity. All the derivatives prepared are active in inhibiting oedema induced by carrageenan. Compound 4e was found more potent with 89% of inhibition followed by compound 4b (86%). Compounds with >70% of anti-inflammatory activity were tested for analgesic, ulcerogenic, and lipid peroxidation profile. Selected compounds were also evaluated for inhibition of COXs (COX-1 and COX-2) and LOXs (LOX-5, LOX-12, and LOX-15). Compound 4e was comparatively selective for COX-2, LOX-5, and LOX-15. Study revealed that these derivatives were more effective than ibuprofen with reduced side effects. It can be suggested that these derivatives could be used to develop more potent and safer NSAIDs.
Journal of Enzyme Inhibition and Medicinal Chemistry 02/2011; 26(6):767-76. · 1.50 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Synthesis of title compounds (4a-j) was carried out by following aminomethylation Mannich reaction. Test compounds were effective in inhibiting edema induced by carrageenan. The percent inhibition obseved was in the range of 25-83.3%. Compound (4c, e, h and j) were also tested for analgesic effect and showed percent protection ranging between 57-65%. All the synthesized compounds were active against E. coli and S. aureus but only compounds (4 b, c, e, i and j) were active against B. subtilis. All these compound were also found active against A. niger. Compound 4j was the most active compound with 83.3% inhibition of edema, 65.35% percent protection and inhibited all the three bacterial strains.
Indian Journal of Pharmaceutical Sciences 01/2011; 73(1):101-4. · 0.30 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: A series of some new benzoxazines derivatives have been synthesized using conventional method and solvent-free microwave thermolysis.
It was observed that the solvent-free microwave thermolysis is a convenient, rapid, high-yielding, and environmental friendly
protocol for the synthesis of benzoxazines when compared with conventional reaction in a solution phase. All the compounds
synthesized were tested for anti-inflammatory activity. Compound 3f, 3h, and 3l showed 74.87, 70.39, and 71.89% of inhibition in rat paw edema, 57.38, 54.27, and 55.47% of protection against acetic acid
induced writhings, and 0.08, 0.17, and 0.17 of severity index (SI), respectively compared to 82.33, 63.06, and 1.0 values
of ibuprofen. The study showed that these compounds are good and safe anti-inflammatory agents and can be used to develop
potent and safe anti-inflammatory agents.