Synthesis and antiallergy activity of N-[2-(dimethylamino)ethyl]-4-aryl-1-piperazinecarboxamide derivatives
作者:David A. Walsh、Jerry B. Green、Stephen K. Franzyshen、Joseph C. Nolan、John M. Yanni
DOI:10.1021/jm00169a037
日期:1990.7
A series of N-[2-(dimethylamino)ethyl]-4-aryl-1-piperazinecarboxamides was synthesized and evaluated for antiallergy activity. Several derivatives had activity in the passive foot anaphylaxis (PFA) assay, an IgE-mediated model useful in the detection of compounds possessing antiallergic activity, but no derivative tested had activity at 10 mg/kg in the guinea pig anaphylaxis (GPA) assay. One analogue, N-[2-(dimethylamino)ethyl]-4-(4-fluorophenyl)-1-piperazinecarboxamide , had an IC50 = 310 nM for inhibition of tritiated mepyramine binding to H1 histaminic receptors isolated from guinea pig cerebral cortex.
Prelog; Blazek, Collection of Czechoslovak Chemical Communications, 1934, vol. 6, p. 549,555
作者:Prelog、Blazek
DOI:——
日期:——
WALSH, DAVID A.;GREEN, JERRY B.;FRANZYSHEN, STEPHEN K.;NOLAN, JOSEPH C.;Y+, J. MED. CHEM., 33,(1990) N, C. 2028-2032
作者:WALSH, DAVID A.、GREEN, JERRY B.、FRANZYSHEN, STEPHEN K.、NOLAN, JOSEPH C.、Y+