1.
Nucleosides Nucleotides Nucleic Acids
; 22(11): 1985-93, 2003 Nov.
Article
in English
| MEDLINE
| ID: mdl-14680021
ABSTRACT
The synthesis of new 3'-deoxy-3'-[4-(pyrimidin-1-yl)methyl-1,2,3-triazol-1-yl]-thymidine 6a-f, from 3'-azido-3'-deoxy-5'-O-monomethoxytrityl-thymidine is described. The key step is the 1,3-dipolar cycloaddition between the azido group of the protected AZT 3 and N-1-propargylpyrimidine derivatives 2a-f. All new derivatives 6a-f were evaluated for their inhibitory effects against the replication of HIV-1 (IIIB), HIV-2 (ROD). No marked activity was found.
Subject(s)
Anti-HIV Agents/chemical synthesis , Thiazoles/chemistry , Thymidine/analogs & derivatives , Anti-HIV Agents/chemistry , Anti-HIV Agents/pharmacology , Cell Line , Cyclization , HIV-1/drug effects , Humans , Structure-Activity Relationship , Thiazoles/chemical synthesis , Thiazoles/metabolism , Thymidine/chemistry
2.
Nucleosides Nucleotides Nucleic Acids
; 20(12): 1949-60, 2001 Dec.
Article
in English
| MEDLINE
| ID: mdl-11794800
ABSTRACT
The synthesis of 1,2,3-triazole acyclonucleosides 7a-h via 1,3-dipolar cycloaddition of N-9/N-1-propargylpurine/pyrimidine 2a-h with azido-pseudo-sugar 4 is described and none of them had anti-HIV activity.