| Abstract
| - A series of 6-aminoquinolone compounds were evaluated for their in vitro activity against humanimmunodeficiency virus type 1 (HIV-1). Compound 12a, bearing a methyl substituent at theN-1 position and a 4-(2-pyridyl)-1-piperazine moiety at the C-7 position, was the most activein inhibiting HIV-1 replication on de novo infected C8166 human lymphoblastoid cell lines.The 12a EC50 value was 0.1 μM, a 7−20-fold lower concentration relative to that for compounds8a and 7a containing a cyclopropyl and tert-butyl substituent at the N-1 position, respectively.When the C-6 amino group was replaced with a fluorine atom, a decreased antiviral effect wasobserved. The observed effects are selective, since potency is substantially reduced when testingthe compounds against the herpes simplex virus type 1 (HSV-1). Active quinolone derivativesvery efficiently interact with TAR RNA, which suggests a nucleic acid-targeted mechanism ofaction.
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