Yasuno, Takumi; Ohe, Tomoyuki; Kataoka, Hiroki; Hashimoto, Kosho; Ishikawa, Yumiko; Furukawa, Keigo; Tateishi, Yasuhiro; Kobayashi, Toi; Takahashi, Kyoko; Nakamura, Shigeo; Mashino, Tadahiko published the artcile< Fullerene derivatives as dual inhibitors of HIV-1 reverse transcriptase and protease>, Electric Literature of 623-50-7 , the main research area is pyridinium fullerene preparation dual inhibitor HIV reverse transcriptase protease; piperidinium fullerene preparation dual inhibitor HIV reverse transcriptase protease; proline fullerene preparation dual inhibitor HIV reverse transcriptase protease; Fullerene; HIV protease; HIV reverse transcriptase.
In the present study, we newly synthesized three types of novel fullerene derivatives: pyridinium-type derivatives, piperidinium-type derivatives, and proline-type derivatives Among the assessed compounds, some 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, 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.
Bioorganic & Medicinal Chemistry Letters published new progress about AIDS (disease). 623-50-7 belongs to class esters-buliding-blocks, and the molecular formula is C4H8O3, Electric Literature of 623-50-7 .
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