Abstract:
:Recently, AZT (N-pyridyl)phosphoramidates were reported as a new type of potential anti-HIV therapeutics. In continuation of that work, here we present new (N-heteroaryl)phosphoramidate derivatives of antiviral 2',3'-dideoxynucleosides containing other types of N-heteroaryl moieties, particularly those with higher lipophilicity. The present studies comprise mechanistic investigations using (31)P NMR correlation analysis, which permitted improvements in the synthetic procedures. The obtained compounds were tested in biological systems to establish their cytotoxicity and anti-HIV activity. The results were analyzed with respect to possible correlations between biological and physico-chemical properties of the phosphoramidates studied, to get some insight into their antiviral mode of action.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Kolodziej K,Romanowska J,Stawinski J,Boryski J,Dabrowska A,Lipniacki A,Piasek A,Kraszewski A,Sobkowski Mdoi
10.1016/j.ejmech.2015.06.004subject
Has Abstractpub_date
2015-07-15 00:00:00pages
77-88eissn
0223-5234issn
1768-3254pii
S0223-5234(15)30079-9journal_volume
100pub_type
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