贝利斯-希尔曼反应辅助平行合成3,5-二取代异恶唑及其作为抗血栓形成剂的体内生物评价。
Baylis-Hillman reaction assisted parallel synthesis of 3,5-disubstituted isoxazoles and their in vivo bioevaluation as antithrombotic agents.
作者信息
Batra S, Roy A K, Patra A, Bhaduri A P, Surin W R, Raghavan S A V, Sharma P, Kapoor K, Dikshit M
机构信息
Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow 226 001, India.
出版信息
Bioorg Med Chem. 2004 May 1;12(9):2059-77. doi: 10.1016/j.bmc.2004.02.023.
The solution-phase parallel synthesis involving reactions of Baylis-Hillman products of 3-substituted-5-isoxazolecarbaldehydes with nucleophiles and their in vivo antithrombotic evaluations are described along with the results of in vitro platelet aggregation inhibition assay of a few compounds. Results of the detailed evaluation of one of the compounds as an inhibitor of platelet aggregation are also presented.
描述了涉及3-取代-5-异恶唑甲醛的贝利斯-希尔曼产物与亲核试剂反应的溶液相平行合成及其体内抗血栓形成评估，以及几种化合物的体外血小板聚集抑制试验结果。还给出了其中一种化合物作为血小板聚集抑制剂的详细评估结果。
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