双苯脒类化合物作为抗真菌剂，是否需要两个脒基功能才能观察到抗卡氏肺孢子虫的活性？

Laboratory of Organic Chemistry, Faculty of Sciences, University of Mons-UMONS, 20 place du parc, B-7000 Mons, Belgium.

Molecules. 2010 Jun 11;15(6):4283-93. doi: 10.3390/molecules15064283.

A library of 19 novel 4-(4-phenylpiperazine-1-yl)benzamidines has been synthesized and evaluated in vitro against Pneumocystis carinii. Among these compounds, N-ethyl- and N-hexyl-4-(4-phenylpiperazine-1-yl)benzamidines emerged as the most promising compounds, with inhibition percentages at 10.0 microg/mL of 87% and 96%, respectively. Those compounds remained active at 0.1 microg/mL.

合成了一个包含 19 种新型 4-(4-苯哌嗪-1-基)苯甲脒的化合物库，并对其进行了体外抗肺囊虫活性评价。在这些化合物中，N-乙基-和 N-己基-4-(4-苯哌嗪-1-基)苯甲脒是最有前途的化合物，其在 10.0μg/mL 时的抑制率分别为 87%和 96%。这些化合物在 0.1μg/mL 时仍具有活性。