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Thiophenes And Furans Derivatives: A New Class Of Potential Pharmacological Agents.

F. Meotti, D. O. Silva, A. S. dos Santos, G. Zeni, J. Rocha, C. Nogueira
Published 2003 · Chemistry, Medicine

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A new class of potential pharmacological thiophenes and furans compounds has been prepared. The obtained thiophenes and furans derivatives were screened for anti-inflammatory, antinociceptive and antioxidant activity in rats. In vitro hepatic ALA-D activity was also evaluated. Thiophene 2 exhibited higher anti-inflammatory effect than thiophenes 1 and 3. However, compound 1 demonstrated lower IC(50) for lipid peroxidation than 2 and 3 in liver and brain. Furan compounds 4-6 presented similar anti-inflammatory activity. The acetylenic furans 4 and 5 inhibited scarcely lipid peroxidation at low concentration as 10 μM. Conversely, furan compound 6 was the most effective against lipid peroxidation in liver. Furans 4 and 5 inhibited lipid peroxidation, in brain, only in high concentrations. In contrast, furan 6 protected (90%) against lipid peroxidation at 10 μM. Thiophene 1 was devoid of anti-inflammatory activity but was efficient in reducing acetic acid-induced constriction. Conversely, it analogue furan 4 presented anti-inflammatory and antinociceptive activity. Thiophene and furan inhibited hepatic ALA-D only at high concentrations. All compounds displayed antioxidant activity however the anti-inflammatory activity is not related to antioxidant potential.
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