RESUMO
Analgesic efficacy was determined by the hot plate method for a group of 17 new pyrazine and 3 non-pyrazine CH and NH acids. The biological data were quantitatively related to the hydrophobicity of the compounds, expressed by fragmental constant, and to the orbital energy of the highest occupied molecular orbital, calculated quantumchemically. It has been found that the higher the electron donating properties, the more active is the agent, provided that its hydrophobicity allows it to reach its site of action. The results obtained support the charge transfer model for the biological interaction of analgesic agents.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Pirazinas/farmacologia , Amidas , Animais , Fenômenos Químicos , Físico-Química , Transporte de Elétrons , Masculino , Camundongos , Nitrilas , Relação Estrutura-AtividadeRESUMO
Condensation reactions of 3-(1H-benzimidazole-2)propanoic acid (procodazol) with aromatic aldehydes were carried out resulting in lactam and acid derivatives. Basing on the spectral studies (MS, NMR) it was found that in the reaction the hydrogen atoms of the 3-methylene group of procodazol take part. 3-[2'-Acetoxyphenyl)methylene]-2,3-dihydro-1 H-pyrrole[1,2-a]benzimidazol-1-one (3c) was found to possess some analgetic properties.
