In the present study, we newly synthesized three types of novel fullerene derivatives: pyridinium-type derivatives trans-3a and 4a-5b, piperidinium-type derivative 9, and proline-type derivatives 10a-12. Among the assessed compounds, 5a, 10e, 10f, 10i, 11a-d, and 12 were found to inhibit both HIV reverse transcriptase and HIV protease (HIV-PR), with IC₅₀ values in the low micromolar range being observed. Regarding HIV-PR inhibition activity, proline-type derivatives 11a-11d and 12, bearing an alkyl chain between the hydroxylmethylcarbonyl (HMC) moiety and pyrrolidine ring, were more potent than other derivatives. This result might indicate that connecting HMC moieties with proline-type fullerene derivatives through properly sized alkyl chain leads to improved HIV-PR inhibitory activity.

在本研究中，我们新合成了三种新型富勒烯衍生物：吡啶鎓型衍生物trans - 3a和4a - 5b，哌啶型衍生物9和脯氨酸型衍生物10a - 12。在评估的化合物中，发现5a，10e，10f，10i，11a - d和12抑制HIV逆转录酶和HIV蛋白酶（HIV-PR），并且IC ₅₀值处于低微摩尔范围。关于HIV-PR的抑制活性，脯氨酸型衍生物在羟甲基羰基（HMC）部分和吡咯烷环之间带有烷基链的11a - 11d和12比其他衍生物更有效。该结果可能表明，通过适当大小的烷基链将HMC部分与脯氨酸型富勒烯衍生物连接会改善HIV-PR的抑制活性。