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Heterocyclic antiinflammatory agents: Structure-activity relationships
242
Pharmacological Research, Vol. 26, Supplement 1, 1992
BETA-BLOCKING PYRIDIN-OXIMINO DERIVATIVES F. Manna, F. Chimenti, A. Bolasco, B. Bizzarri, R. Lena, A. Filippelli, A. Palla, M. Costantino, F. Rossi Dep. St. Chem. and Tech. Biol. Act. Sub. University of Rome "La Sapienza"Rome, Italy - In. Pharm. Tox. I Fat. Med. SW. Univ. Naples, Naples, Italy
Pyridin-oximino derivatives which showed p-blocking activity were synthesized. In order to study the structure-activity relationships, some substituents were introduced in the pyridine ring (CH3, Ph). The effects produced by several amines in the side chain were also investigated. Stereoselective synthesis was performed and gave a mixture of the enantiomers with enantiomeric ratio of 7~3. Pharmacological activity of the enantiomeric forms compared with the racemic compound didn't show any particular b-selectivity. The replacement of the pyridine ring with 3-indolyl moiety and the intercalation of an imino bond produced in some derivatives good b-blocking activity.
HETEROCYCLIC ANTIINFLAMMATORY AGENTS: STRUCTURE-ACTIVITY RELATIONSHIPS E.Abignente,F.Arena,P.De Caprariis,E.Luraschi,A.Sacchi,C.Saturnino,M.G.Ri moli,F.Rossi,E.Lampa,L.Berrino Dip.Chimica Farmaceutica,Facoltl di Farmacia, and Istituto di Farmacologia, I Facolta di Medicina e Chirurgia - Universita di Napoli "Federico II” We have taken into consideration a group of heterocyclic systems characte rized by an imidazole ring fused with another heterocyclic ring as a toolto study the mechanisms of action involved in the antiinflaaznatory and a! algesic activity of non-steroidal compounds and their structure-activity relationships. Host of new compounds till now synthesized, which are all related to an only structural model (imidazopyridines, imidazopyrimidines. imidazopyrazi nes, imidazopyridazines, imidazothiazoles. imidazobenzothiazoles), showed: a) significant antiinflarmaatory and/or analgesic activity; b) low or negll gible ulcerogenic action on the gastric mucosa; c1 more or less remarkable In some cases it inhibitory activity on the prostaglandin biosynthesis. was possible to point out clear structure-activity relationships (1). (1)
E.Abignente, (1991).
ActuaZit&
de Chtiie
fibapeutique,
186me Serie,
193-214
Pharmacological Research, Vol. 26, Supplement 1, 1992
BETA-BLOCKING PYRIDIN-OXIMINO DERIVATIVES F. Manna, F. Chimenti, A. Bolasco, B. Bizzarri, R. Lena, A. Filippelli, A. Palla, M. Costantino, F. Rossi Dep. St. Chem. and Tech. Biol. Act. Sub. University of Rome "La Sapienza"Rome, Italy - In. Pharm. Tox. I Fat. Med. SW. Univ. Naples, Naples, Italy
Pyridin-oximino derivatives which showed p-blocking activity were synthesized. In order to study the structure-activity relationships, some substituents were introduced in the pyridine ring (CH3, Ph). The effects produced by several amines in the side chain were also investigated. Stereoselective synthesis was performed and gave a mixture of the enantiomers with enantiomeric ratio of 7~3. Pharmacological activity of the enantiomeric forms compared with the racemic compound didn't show any particular b-selectivity. The replacement of the pyridine ring with 3-indolyl moiety and the intercalation of an imino bond produced in some derivatives good b-blocking activity.
HETEROCYCLIC ANTIINFLAMMATORY AGENTS: STRUCTURE-ACTIVITY RELATIONSHIPS E.Abignente,F.Arena,P.De Caprariis,E.Luraschi,A.Sacchi,C.Saturnino,M.G.Ri moli,F.Rossi,E.Lampa,L.Berrino Dip.Chimica Farmaceutica,Facoltl di Farmacia, and Istituto di Farmacologia, I Facolta di Medicina e Chirurgia - Universita di Napoli "Federico II” We have taken into consideration a group of heterocyclic systems characte rized by an imidazole ring fused with another heterocyclic ring as a toolto study the mechanisms of action involved in the antiinflaaznatory and a! algesic activity of non-steroidal compounds and their structure-activity relationships. Host of new compounds till now synthesized, which are all related to an only structural model (imidazopyridines, imidazopyrimidines. imidazopyrazi nes, imidazopyridazines, imidazothiazoles. imidazobenzothiazoles), showed: a) significant antiinflarmaatory and/or analgesic activity; b) low or negll gible ulcerogenic action on the gastric mucosa; c1 more or less remarkable In some cases it inhibitory activity on the prostaglandin biosynthesis. was possible to point out clear structure-activity relationships (1). (1)
E.Abignente, (1991).
ActuaZit&
de Chtiie
fibapeutique,
186me Serie,
193-214