Poite,M.; Metzger,J., Bulletin de la Societe Chimique de France, 1962, p. 2078 - 2085
作者:Poite,M.、Metzger,J.
DOI:——
日期:——
Preparation of thiazoles
申请人:WINGFOOT CORP
公开号:US02263014A1
公开(公告)日:1941-11-18
Analogs of platelet activating factor. 6. Mono- and bis-aryl phosphate antagonists of platelet activating factor
作者:A. Wissner、M. L. Carroll、K. E. Green、S. S. Kerwar、W. C. Pickett、R. E. Schaub、L. W. Torley、S. Wrenn、C. A. Kohler
DOI:10.1021/jm00087a023
日期:1992.5
A series of aryl phosphoglyceride (3, 19-6 1) and bis-aryl phosphate (67-135) antagonists of platelet activating factor (PAF) were prepared. A group of four bifunctional phosphorus reagents (5a-c and 7) were developed that allowed the preparation of these aryl phosphates in which the position of aromatic substitution can be varied. These compounds were examined for their ability to inhibit PAF-induced platelet aggregation of rabbit platelets. Selected compounds were also evaluated for their ability to displace [H-3]PAF from its receptor on rabbit platelets. These in vitro data were compared to similar data obtained for a number of known PAF antagonists. The compounds were evaluated in vivo, in both the mouse and rabbit, for their ability to prevent death induced by a lethal challenge of PAF. The relationships between the biological activity and the nature, lipophilicity, and position of substituents of the aromatic rings were studied. Compound 105 (CL 184005) has been selected to undergo further development as a potential therapeutic agent for the treatment of septic shock in man.
Ganapathi; Venkataraman, Proceedings - Indian Academy of Sciences, Section A, 1945, # 22, p. 362,376
作者:Ganapathi、Venkataraman
DOI:——
日期:——
Hydrogen–deuterium exchange in thiazoles via phase-transfer catalysis
作者:William J. Spillane、Patrick Kavanagh、Frances Young、Henri J.-M. Dou、Jacques Metzger
DOI:10.1039/p19810001763
日期:——
quaternary (ammonium, phosphonium, and arsonium) salts and 17 solvents have been studied. The effect of chain-length of the salt [Me(CH2)n]4[graphic omitted]Br–(n= 1–5) has been examined. First-order kinetics (in thiazole) are reported for seven thiazoles. The present method offers a practical route to specifically and higher deuteriated (D 90%) thiazoles and other aromatics.