Synthesis and quantitative structure–activity relationship study of substituted imidazophosphor ester based tetrazolo[1,5-b]pyridazines as antinociceptive/anti-inflammatory agents

• Wafaa M. Abdou,
• Neven A. Ganoub and
• Eman Sabry

Beilstein J. Org. Chem. 2013, 9, 1730–1736, doi:10.3762/bjoc.9.199

• our products. Antinociceptive evaluation para-Benzoquinone (p-BQ)-induced writhing test The evaluation of antinociceptive activity of the synthesized compounds was assessed in vivo in mice by using the p-benzoquinone-induced writhing test [26]. Ibuprofen was used as a positive control in our

• , while the azido substrate 1 showed only a weak antinociceptive effect (14%), the eight phosphor compounds demonstrated higher capacity than the reference ibuprofen drug (69.9%) at the same dose of 50 mg per kilogram body weight. Anti-inflammatory screening Carrageenan-induced hind paw edema test Anti

• the most antinociceptive/anti-inflammatory activity, even higher than the references ibuprofen and indomethacin; (2) there is a parallel correlation between the anti-inflammatory activities and the antinociceptive activity results (Table 1); (3) the amino group substituent has a positive effect (see 7

The conjugation of nonsteroidal anti-inflammatory drugs (NSAID) to small peptides for generating multifunctional supramolecular nanofibers/hydrogels

• Jiayang Li,
• Yi Kuang,
• Junfeng Shi,
• Yuan Gao,
• Jie Zhou and
• Bing Xu

Beilstein J. Org. Chem. 2013, 9, 908–917, doi:10.3762/bjoc.9.104

• acting as a general motif, enables enzymatic hydrogelation in which the precursor turns into a hydrogelator upon hydrolysis catalyzed by a phosphatase at physiological conditions. The conjugates of Phe–Phe with other NSAIDs, such as (R)-flurbiprofen (2), racemic flurbiprofen (3), and racemic ibuprofen (4

• phosphatase and results in a hydrogel of 1d under physiological conditions. In addition to naproxen, we evaluate the abilities of other NSAIDs (Scheme 1) as building blocks of hydrogelators and find that the conjugates of FF and (R)-flurbiprofen (2), racemic flurbiprofen (3) or racemic ibuprofen (4) form

• -enantiomer 2 or racemic 3) conjugates with L- or D-diphenylalanine to afford compounds (R)-Fbp-FF (2a), (R)-Fbp-ff (2b), and (RS)-Fbp-FF (3a) (Fbp = flurbiprofen). The attachment of racemic ibuprofen to L-diphenylalanine yields compound (RS)-Ibp-FF (4a) (Ibp = ibuprofen). Since the direct use of

Functionalization of heterocyclic compounds using polyfunctional magnesium and zinc reagents

• Paul Knochel,
• Matthias A. Schade,
• Sebastian Bernhardt,
• Georg Manolikakes,
• Albrecht Metzger,
• Fabian M. Piller,
• Christoph J. Rohbogner and
• Marc Mosrin

Beilstein J. Org. Chem. 2011, 7, 1261–1277, doi:10.3762/bjoc.7.147

• the synthesis of the blockbuster drug ibuprofen (170). To achieve this, the secondary benzylic zinc reagent 169 was reacted with CO2 gas to provide the phenylacetic acid 170 in 89% yield. Conclusion We have summarized the most important procedures for the preparation of functionalized organzinc and

An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

• Marcus Baumann,
• Ian R. Baxendale,
• Steven V. Ley and
• Nikzad Nikbin

Beilstein J. Org. Chem. 2011, 7, 442–495, doi:10.3762/bjoc.7.57

• Selective inhibitors of cyclooxygenase-2 (COX-2) are widely used for their anti-inflammatory effects and have shown less gastrointestinal side effects when compared to other anti-inflammatory agents, notably non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin and ibuprofen, which inhibit both COX

Miniemulsion polymerization as a versatile tool for the synthesis of functionalized polymers

• Daniel Crespy and
• Katharina Landfester

Beilstein J. Org. Chem. 2010, 6, 1132–1148, doi:10.3762/bjoc.6.130

• encapsulation of ibuprofen [115]. Interfacial polyaddition in inverse miniemulsions is becoming especially popular since it allows the encapsulation of hydrophilic substances in various polymeric capsules. The method allows the formation of particles with capsular morphology consisting of a liquid core and a