Synthesis of 5-beta-D-ribofuranosylnicotinamide and its N-methyl derivative. The isosteric and isoelectronic analogues of nicotinamide nucleoside.
Synthesis of 5-beta-D-ribofuranosylnicotinamide and its N-methyl derivative. The isosteric and isoelectronic analogues of nicotinamide nucleoside.
复制标题
5-β-D-呋喃核糖基烟酰胺及其N-甲基衍生物的合成。
DOI：
10.1021/jm00388a030
复制
发表时间：
1987
影响因子：
7.3
通讯作者：
Watanabe,KA
中科院分区：
文献类型：
--
作者：
Kabat,MM;Pankiewicz,KW;Watanabe,KA
(42) Born, G. VR Nature (London) 1962, 194, 927. a 3-min time course. Citrated human platelet-rich plasma from normal, healthy donors who denied receiving any medication for 10 days was purchased from a commercial blood bank. The plasma was centrifuged at 164g to remove any remaining red blood cells and maintained at 25 C until the experiments were performed. The antagonists were dissolved in 50% ethanol/normal saline and then added as 10-µ aliquotsper 1 mL of platelet-rich plasma to give the specified concentration 3 min before being challenged with U46619 (3 µ). Inhibition was measured as a percentage of control bloods that had not received any drug. The ED50 values were estimated from three to four concentrations of drug that gave inhibition in the range of 10-90%. Dark and Light Inhibition Studies of Aromatic Azides. 13-Azaprostanoic acid, or one of the three derivatives listed in Table II, was added to platelet-rich plasma at the minimum concentration necessary to produce 100% inhibition of 3 µ U46619-induced aggregation. The incubates were photolyzed (30 min) with a HBD100W OSRAM mercury light. This extended photolysis time was necessary because of the high UV absorption by the plasma. The platelets were then centrifuged and the platelet pellet resuspended in Tris-HCl buffer (pH 7.4). Platelet aggregation of the resuspended cells was induced by addition of ADP (10 µ) or U46619 (0.5 µ). The results are presented in Table II, where the values were calculated by the following re-lationship: percent inhibition relativeto 13-azaprostanoic acid=[1-(residual plateletactivity with given azide/the residual platelet activity with 13-azaprostanoic acid)] X 100. Acknowledgment. This work was supported by the National Institutes of Health (HL 24530). U46619 was kindly provided by Dr. Gordon L. Bundy of the Upjohn Co., Kalamazoo, MI. The investigators acknowledge the Research Resources Center at the University of Illinois at Chicago for providing in part the instrumentation used in this study and Lolita Strebel for technical assistance in the aggregation studies.
