Non-steroidal antiinflammatory agents. Synthesis and enzyme inhibition of 2-[4-(heteroarylmethyl)phenyl] propanoic acids and analogues.
Some 2-[4-(heteroarylmethyl)phenyl]propanoic acids and phenylacetic and benzoic analogues has been synthesized. All above acids were tested for their inhibitory activity on lipoxygenase and cyclooxygenase, in comparison with NDGA and tolmetin. 2-[4-(Thien-2-ylmethyl)phenyl]propanoic acid 2, strictly related with suprofen, was found the most interesting compound, giving rise to a 79% inhibition of the cyclooxygenase activity at 10(-4) M concentration.
Silvestri
R
R
Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, Italy.
Pagnozzi
E
E
Valoti
M
M
Fusi
F
F
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D016859:Lipoxygenase Inhibitors