Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents.
Phosphonated carbocyclic 2'-oxa-3'-azanucleosides have been synthesized and tested for their antiretroviral activity. The obtained results have shown that some of the compounds were as powerful as azydothymidine in inhibiting the reverse transcriptase activity of the human retrovirus T-cell leukemia/lymphotropic virus type 1 and in protecting human peripheral blood mononuclear cells against human retrovirus T-cell leukemia/lymphotropic virus type 1 transmission in vitro. These data indicate that phosphonated carbocyclic 2'-oxa-3'-azanucleosides possess the necessary requirements to efficiently counteract infections caused by human retroviruses.
Chiacchio
Ugo
U
Dipartimento di Scienze Chimiche, Università di Catania, Viale Andrea Doria 6, Catania 95125, Italy.
Rescifina
Antonio
A
Iannazzo
Daniela
D
Piperno
Anna
A
Romeo
Roberto
R
Borrello
Luisa
L
Sciortino
Maria Teresa
MT
Balestrieri
Emanuela
E
Macchi
Beatrice
B
Mastino
Antonio
A
Romeo
Giovanni
G
D044966:Anti-Retroviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015368:Human T-lymphotropic virus 1 / Q000187:drug effects* / Q000201:enzymology / Q000472:pathogenicity; D006801:Humans; D066298:In Vitro Techniques; D007963:Leukocytes, Mononuclear / Q000187:drug effects / Q000821:virology; D063065:Organophosphonates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011684:Purine Nucleosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011741:Pyrimidine Nucleosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D044966:Anti-Retroviral Agents; D001372:Aza Compounds; D063065:Organophosphonates; D011684:Purine Nucleosides; D011741:Pyrimidine Nucleosides; D018894:Reverse Transcriptase Inhibitors