Wikel J H, Paget C J, DeLong D C, Nelson J D, Wu C Y, Paschal J W, Dinner A, Templeton R J, Chaney M O, Jones N D, Chamberlin J W
J Med Chem. 1980 Apr;23(4):368-72. doi: 10.1021/jm00178a004.
The synthesis and antirhinovirus activity of syn and anti isomers of 6-[[(hydroxyimino)phenyl]methyl]-1-[(1-methylethyl)sulfonyl]-1H-benzimidazol-2-amine (4 and 5) are reported. The structural assignments of 4 and 5 are based upon 13C NMR spectra of both isomers and also X-ray analysis of 5. The anti-isomer 5 was more potent than the syn-isomer 4 when compared as an inhibitor of rhinovirus multiplication in vitro. Both isomers inhibited multiplication of 15 different serotypes of rhinovirus.
报道了6-[[(羟基亚氨基)苯基]甲基]-1-[(1-甲基乙基)磺酰基]-1H-苯并咪唑-2-胺（4和5）的顺式和反式异构体的合成及其抗鼻病毒活性。4和5的结构归属基于两种异构体的13C NMR光谱以及5的X射线分析。在体外作为鼻病毒增殖抑制剂进行比较时，反式异构体5比顺式异构体4更有效。两种异构体均抑制15种不同血清型鼻病毒的增殖。
