Walker K A, Sjogren E B, Matthews T R
J Med Chem. 1985 Nov;28(11):1673-9. doi: 10.1021/jm00149a023.
Screening of mesoionic compounds as potential electron acceptors by analogy with metronidazole led to the finding of in vitro antitrichomonal activity for anhydro-2-phenyl-3-hydroxythiazolo [3,2-a]pyridinium hydroxide (1). In a series of analogues, potent in vitro activity was found to be associated with amino substitution; however, such activity was dependent on specific structural features and not on the reduction potential. The most active compounds showed only poor in vivo activity.
通过与甲硝唑类比筛选作为潜在电子受体的中氮茚化合物，发现了无水-2-苯基-3-羟基噻唑并[3,2-a]吡啶氢氧化合物（1）的体外抗滴虫活性。在一系列类似物中，发现体外强效活性与氨基取代有关；然而，这种活性取决于特定的结构特征而非还原电位。活性最强的化合物在体内仅表现出较差的活性。
