Synthesis of new 1-phenyl-3-{4-[(2E)-3-phenylprop-2-enoyl]phenyl}-thiourea and urea derivatives with anti-nociceptive activity.
Chalcones or 1,3-diaryl-2-propen-1-ones are known to be useful for treating pain, inflammation, and certain diseases although their uses have not been scientifically verified. Due to the limitations of opioid and NSAID therapy, there is a continuing search for new analgesics. A series of novel new 1-phenyl-3-{4-[(2E)-3-phenylprop-2-enoyl]phenyl}-thiourea and urea derivatives were synthesized and evaluated against writhing test in mice, following the aromatic substitution pattern proposed by Topliss. The results of the preliminary bioassays indicate that compound 3 presents promising anti-nociceptive activity in acetic acid-, formalin-, and glutamate-induced pain in mice, compared with some well-known non-steroidal anti-inflammatory and analgesic drugs.
dos Santos
Lorena
L
Departamento de Química, Curso de Pós-Graduação em Química, Universidade Federal de Santa Catarina/UFSC, Florianópolis, Santa Catarina, Brazil. lorennasantos@gmail.com
Lima
Luíse Azevedo
LA
Cechinel-Filho
Valdir
V
Corrêa
Rogério
R
de Campos Buzzi
Fátima
F
Nunes
Ricardo José
RJ
D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology*; D001681:Biological Assay; D051379:Mice; D010147:Pain Measurement; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D014508:Urea / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D014508:Urea; D013890:Thiourea