Buckler R T, Hartzler H E, Kurchacova E, Nichols G, Phillips B M
J Med Chem. 1978 Dec;21(12):1254-60. doi: 10.1021/jm00210a015.
All possible "nonadjacent" phenyltriazolepropionic acids were synthesized and tested for antiinflammatory activity. Two of the isomers displayed activity approximately equal to phenylbutazone: the 4-phenyl-1,2,3,-triazole-2-propionic acid (7) and its reverse counterpart, 2-phenyl-1,2,3-triazole-4-propionic acid (6). The other five isomers were inactive. Since these seven acids are geometrically congruent and possess similar lipophilic characters, antiinflammatory activity must depend on some property that is a function of how the carbon and nitrogen atoms are arranged in the triazole ring.
合成了所有可能的“非相邻”苯基三唑丙酸，并对其抗炎活性进行了测试。其中两种异构体的活性与保泰松大致相当：4-苯基-1,2,3-三唑-2-丙酸（7）及其反向异构体2-苯基-1,2,3-三唑-4-丙酸（6）。其他五种异构体无活性。由于这七种酸在几何结构上是全等的，并且具有相似的亲脂性，因此抗炎活性必定取决于三唑环中碳和氮原子排列方式所决定的某些性质。
