Fullerene derivatives as dual inhibitors of HIV-1 reverse transcriptase and protease
نویسندگان
چکیده
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, proline-type 10a-12. Among assessed compounds, 5a, 10e, 10f, 10i, 11a-d, 12 were found to inhibit both HIV reverse transcriptase protease (HIV-PR), with IC50 values in low micromolar range being observed. Regarding HIV-PR inhibition activity, 11a-11d 12, bearing an alkyl chain between hydroxylmethylcarbonyl (HMC) moiety pyrrolidine ring, more potent than other derivatives. This result might indicate that connecting HMC moieties through properly sized leads improved inhibitory activity.
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2021
ISSN: ['1464-3405', '0960-894X']
DOI: https://doi.org/10.1016/j.bmcl.2020.127675