Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.

The cyclic enaminone moiety has been identified as a new scaffold for selective inhibition of cyclooxygenase-2 with anti-inflammatory and analgesic activities. The designed cyclic enaminones have been synthesized conveniently through the development of a new catalyst-free methodology and evaluated for cyclooxygenase (COX-1 and COX-2) inhibitory activities. Three compounds 7d, 8, and 9 predominantly inhibited COX-2 with selectivity index of 74.

2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.

The 2-(2-arylphenyl)benzoxazole moiety has been found to be a new and selective ligand for the enzyme cyclooxygenase-2 (COX-2). The 2-(2-arylphenyl)benzoxazoles 3a-m have been synthesized by Suzuki reaction of 2-(2-bromophenyl)benzoxazole. Further synthetic manipulation of 3f and 3i led to 3o and 3n, respectively.

Optimization of extrusion conditions for defatted soy-rice blend extrudates.

Processing parameters of feed including moisture content of feed (12, 15, 18, 21 and 24%), soy flour-rice blend ratio (10:90, 14:86, 18:82, 22:78 and 26:74), operational parameters of extruder like barrel temperature (100, 110, 120, 130 and 140 °C), die head temperature (160, 170, 180, 190 and 200 °C) and screw speed (100, 110, 120, 130 and 140 rpm) were optimized for physical and textural properties of soy-rice blend extrudates. The minimum value of longitudinal expansion index lied near 185 °C die head temperature at about 120 rpm. The minimum value of bulk density was observed in between 18:82 blend ratio and 115 °C barrel temperature.

Progress in COX-2 inhibitors: a journey so far.

The non-steroidal anti-inflammatory drugs (NSAIDs) are diverse group of compounds used for the treatment of inflammation, since the introduction of acetylsalicylic acid in 1899. Traditional (first generation) NSAIDs exert antiinflammatory, analgesic, and antipyretic effects through the blockade of prostaglandin synthesis via non-selective inhibition of cyclooxygenase (COX-1 and COX-2) isozymes. Their use is associated with side effects such as gastrointestinal and renal toxicity.