Thermosettable compounds prepared from monohydroxy aromatic aldehydes and methylated pyridines or pyrazines
申请人:THE DOW CHEMICAL COMPANY
公开号:EP0212095A1
公开(公告)日:1987-03-04
Thermostable compounds are prepared by reacting methylated pyridines and/or pyrazines with one or more monohydroxy aromatic aldehydes having the ortho and para positions to the hydroxy group block with groups inert to condensation reactions. These compounds are useful to make unsaturated derivatives which can cure into high temperature resistant polymers and/or laminates without giving off condensation products.
Effect of structure on potency and selectivity in 2,6-disubstituted-4-(2-arylethenyl)phenol lipoxygenase inhibitors
作者:Edward S. Lazer、Hin Chor Wong、Craig D. Wegner、Anne G. Graham、Peter R. Farina
DOI:10.1021/jm00169a010
日期:1990.7
A series of 2,6-disubstituted 4-(2-arylethenyl)phenols with potent human neutrophil 5-lipoxygenase (5-LO) inhibiting activity (IC50S in the 10(-7) M range) and weaker human platelet cyclooxygenase (CO) inhibiting activity (IC50S in the 10(-6) M range) is described. This series evolved from the chemical modification of an antiinflammatory dual CO/5-LO inhibitor, 2,6-di-tert-butyl-4-[2-(3-pyridyl)ethenyl]phenol (BI-L-93 BS). The potency and selectivity for 5-LO inhibition is greatly influenced by the nature of the substituents in the 2- and 6-positions. Other structure-activity relationships that determine relative 5-LO and CO potency are discussed. In vivo activity against antigen-induced leukotriene-mediated bronchoconstriction and cell influx in guinea pigs is presented. Representatives of the series are active when administered at 30 mg/kg ip.
LAZER, EDWARD S.;WONG, HIN-CHOR;WEGNER, GRAIG D.;GRAHAM, ANNE G.;FARINA, +, J. MED. CHEM., 33,(1990) N, C. 1892-1898
作者:LAZER, EDWARD S.、WONG, HIN-CHOR、WEGNER, GRAIG D.、GRAHAM, ANNE G.、FARINA, +