Flavonoids are phytochemical compounds found in a variety of plants, fruits, vegetables, leaves, and barks, it offers a wide range of
health benefits. Quercetin is a polyphenolic flavonoid that is found in onions, apples, berries, broccoli, grapes, nuts, cherries and many
other food products. Pharmacologically, quercetin has been examined for various disorders and is reported to possess the ability to prevent as well as treat them. It possesses anti-oxidant, anti-allergic, anti-inflammatory, anti-viral and anti-cancer activity as well. Developing suitable formulation for the delivery of quercetin to specific site leads to better compliance and effective treatment of the disease. This review article highlights the beneficiary activities exhibited by quercetin along with the mechanism behind its activity, followed by reporting the different quercetin formulations developed in last few years.
To obtain selective and potent opioid receptor ligands, we synthesized dehydro derivatives of alvimopan and found compound (28f), a selective but modest affinity MOR antagonist weaker than alvimopan (1). We replaced the arylpiperidine unit by an arylpiperazine to obtain the 1-(α-carboxycinnamyl)-4-arylpiperazines like 13h, which to our surprise had no MOR or DOR activity but was a KOR agonist with moderate affinity. In contrast, literature examples of arylpiperazines 4 and 5 were reported to be pan opioid receptor antagonists, while 6 was a MOR agonist. Two compounds (13l and 11b) showed analgesic response in tail flick test which was blocked by pretreatment with norbinaltorphimine (norBNI). Among 10 1-(α-carboxycinnamyl)-4-arylpiperidines, compound 28g and five others were specific MOR antagonists. Interestingly, compound 26b of this series was found to be more potent than naloxone but weaker than 1. Docking studies have explained differential activities of the above piperazines and piperidines.
An Efficient Scale up Process for Synthesis of N-Arylpiperazines. -An efficient protocol for the synthesis of various substituted phenylpiperazines is presented using sulfolane as solvent. The procedure is clean, high yielding and products are obtained in high purities (>99%). It is also fast and convenient, as the final products are precipitated as the hydrochloride salts and can be isolated by filtration. -(RAVILLA, L.; SUBBA NAIDU, N. V.; NAGARAJAN*, K.; Tetrahedron Lett. 56 (2015) 30, 4541-4544, http://dx.
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