Thalidomide analogues: Tumor necrosis factor-alpha inhibitors and their evaluation as anti-inflammatory agents

JUAN JOSÉ CASAL; ANA MARÍA BRUNO; MARÍA ELISA LOMBARDO; MARIELA BOLLINI

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2016 vol. 83 p. 114 - 119

0928-0987

A series of related Thalidomide derivatives have been synthesized by microwave irradiation and evaluated for anti-inflammatory activity. Anti-inflammatory activity of the tested compounds was performed in vivo, in vitro and ex vivo. Compounds 2, 8 and 9 showed the highest levels of inhibition of TNF-α production. On rat paw edema and hyperalgesia assays compound 9, (1,4-phthalazinedione) demonstrated the highest in vivo anti-inflammatory activity. Thus, compound 9 is considered as a promising compound for further modification to obtain new agents for the treatment of inflammatory diseases.