Antimicrobial Agents and Chemotherapy · 1999 · 31 citations · 21 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryOrganic ChemistryStructure-activity RelationshipsAntiretroviral TherapyAntiviral AgentsAntiviral PharmacologyAntiviral ResistanceAntiviral TherapyHeterocyclic ChemistryAntiviral Structure-activity RelationshipsCell-based AssaysHiv Antiretroviral TherapyNucleoside AnalogsNucleoside Analogue AntiviralsNucleoside Analogue TherapyNucleoside Reverse Transcriptase Inhibitors
Nucleoside analogues with a Z- or an E-methylenecyclopropane moiety were synthesized and examined for activity against human immunodeficiency virus type 1 (HIV-1) in vitro. The addition of a methyl phenyl phosphoro-L-alaninate moiety to modestly active analogues resulted in potentiation of their anti-HIV-1 activity. Two such compounds, designated QYL-685 (with 2,6-diaminopurine) and QYL-609 (with adenine), were most potent against HIV-1 in vitro, with 50% inhibitory concentrations of 0.034 and 0.0026 microM, respectively, in MT-2 cell-based assays. Both compounds were active against zidovudine-resistant, didanosine-resistant, and multi-dideoxynucleoside-resistant infectious clones in vitro. Further development of these analogues as potential therapies for HIV-1 infection is warranted.
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Isolation of a New Human Retrovirus from West African Patients with AIDS
François Clavel, Denise Guétard, Françoise Brun‐Vézinet et al. · Science · 1986 · 1.3K citations
T Shirasaka, Mark F. Kavlick, Takamasa Ueno et al. · Proceedings of the National Academy of Sciences · 1995 · 390 citations