Synthesis and anticonvulsant activity of N-(benzoylalkyl)imidazoles and N-(.omega.-phenyl-.omega.-hydroxyalkyl)imidazoles
摘要:
A novel series of N-(benzoylalkyl)imidazoles and N-(omega-phenyl-omega-hydroxyalkyl)imidazoles was synthesized and evaluated for anticonvulsant activity in mice against maximal electroshock induced seizures. Some of the compounds showed an activity comparable to or better than phenytoin and phenobarbital. The N-[beta-[4-(beta-phenylethyl)phenyl]-beta-hydroxyethyl]imidazole (38) was selected for further studies; preclinical toxicology and additional efficacy evaluations are in progress. Structure-activity relationships are discussed.
Synthesis and anticonvulsant activity of N-(benzoylalkyl)imidazoles and N-(.omega.-phenyl-.omega.-hydroxyalkyl)imidazoles
摘要:
A novel series of N-(benzoylalkyl)imidazoles and N-(omega-phenyl-omega-hydroxyalkyl)imidazoles was synthesized and evaluated for anticonvulsant activity in mice against maximal electroshock induced seizures. Some of the compounds showed an activity comparable to or better than phenytoin and phenobarbital. The N-[beta-[4-(beta-phenylethyl)phenyl]-beta-hydroxyethyl]imidazole (38) was selected for further studies; preclinical toxicology and additional efficacy evaluations are in progress. Structure-activity relationships are discussed.
Hydroxyethyl-azole, Verfahren zu ihrer Herstellung sowie ihre Verwendung als Arzneimittel
申请人:BAYER AG
公开号:EP0011769A1
公开(公告)日:1980-06-11
Hydroxyethyl-azole der allgemeinen Formel
in welcher
Az für Imidazol oder Triazol steht,
R für gegebenenfalls substituiertes Phenly, Naphthyl oder Tetrahydronaphthyl steht,
R1 für gegebenenfalls substituiertes Phenyl oder Cycloalkyl steht und
R2 für Wasserstoff steht oder
R' und R2 gemeinsam in o-Stellung zueinander für eine gegebenenfalls substituierte, mehrgliedrige Methylenbrücke oder zusammen mit dem Phenylring für Naphthyl stehen,
R3 für Halogen, Alkyl, Alkoxy oder Halogenalkyl steht und
n für 0, 1, 2 oder 3 steht,
weisen antimykotische Eigenschaften auf.
通式如下的羟乙基唑
其中
Az 是咪唑或三唑、
R 是任选取代的苯基、萘基或四氢萘基、
R1 代表任选取代的苯基或环烷基,以及
R2 是氢或
R' 和 R2 在彼此相对的 o 位上代表任选取代的多元亚甲基桥,或与苯基环一起代表萘基、
R3 代表卤素、烷基、烷氧基或卤代烷基,以及
n 为 0、1、2 或 3、
具有抗真菌特性。
Hydroxypropyl-imidazole, Verfahren zu ihrer Herstellung sowie diese enthaltende Arzneimittel
申请人:BAYER AG
公开号:EP0005250B1
公开(公告)日:1981-08-12
NARDI, D.;TAJANA, A.;LEONARDI, A.;PENNINI, R.;PORTIOLI, F.;MAGISTRETTI, M+, J. MED. CHEM., 1981, 24, N 6, 727-731
Synthesis and anticonvulsant activity of N-(benzoylalkyl)imidazoles and N-(.omega.-phenyl-.omega.-hydroxyalkyl)imidazoles
作者:Dante Nardi、Alberto Tajana、Amedeo Leonardi、Renzo Pennini、Ferruccio Portioli、Maria Jose Magistretti、Alessandro Subissi
DOI:10.1021/jm00138a017
日期:1981.6
A novel series of N-(benzoylalkyl)imidazoles and N-(omega-phenyl-omega-hydroxyalkyl)imidazoles was synthesized and evaluated for anticonvulsant activity in mice against maximal electroshock induced seizures. Some of the compounds showed an activity comparable to or better than phenytoin and phenobarbital. The N-[beta-[4-(beta-phenylethyl)phenyl]-beta-hydroxyethyl]imidazole (38) was selected for further studies; preclinical toxicology and additional efficacy evaluations are in progress. Structure-activity relationships are discussed.