Page
%P
12 Result(s)
-
Article
Synthesis and anti-HIV evaluation of new 2-Thioxoimidazolidin-4-ones and their Arylidine (styryl) derivatives
1,3-Bis{(2-thiophene-2-yl)ethyl}-5-(arylidine)-2-thioxoimidazolidin-4-ones (5a – 5 m) have been synthesized by condensation of 1,3-diarylalkyl-2-thiohydantoin (4) with various aromatic aldehydes. Compound (4) was...
-
Chapter
Antiviral Agents Acting as DNA or RNA Chain Terminators
Nucleoside or nucleotide analogue inhibitors of viral replication almost act as chain terminators during DNA (DNA- and retroviruses) or RNA (RNA viruses) synthesis. Following intracellular phosphorylation, by ...
-
Article
Carrier Mechanisms Involved in the Transepithelial Transport of bis(POM)-PMEA and Its Metabolites Across Caco-2 Monolayers
Purpose. To investigate the role of carrier mechanisms in: [1] the polarized transport of the bis(pivaloyloxymethyl)- [bis(POM)-] ester prodrug of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine [PMEA] a...
-
Article
Comparison of the Disposition of Ester Prodrugs of the Antiviral Agent 9-(2-phosphonylmethoxyethyl)adenine [PMEA] in Caco-2 Monolayers
Purpose. To evaluate the potential of several bis-ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA, adefovir) to enhance the oral absorption of PMEA.
-
Chapter
Metabolism of Eicar (5-Ethynyl-1-β-D- Ribofuranosylimidazole-4-Carboxamide),A Potent Inhibitor of Inosinate Dehydrogenase
The cytostatic agent 5-ethynyl-l-β-D-ribofuranosylimidazole-4-carboxamide (EICAR) causes a rapid and marked inhibition of inosinate (IMP) dehydrogenase activity in intact tumor cells. [3H]EICAR is metabolised in ...
-
Chapter
Metabolism and Anti-HIV Activity of Phosphoramidate Derivatives of D4T-MP with Variations in the Amino Acid Moiety
The metabolism of different phosphoramidate prodrugs of d4T-MP, in which the phosphate group is linked to a phenyl group and the alkyl ester of an amino acid was studied in crude CEM cell extracts. Significant...
-
Chapter
In Vitro and in Vivo Inhibitory Activity of the Differentiation-Inducing Agent 9-(2-Phosphonylmethoxyethyl)Adenine (Pmea) Against Rat Choriocarcinoma
The acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl)adenine (PMEA) has previously been shown to be a strong inducer of differentiation in several tumor cell lines. We have now investigated the in vitro
-
Chapter
Inhibition of HIV Replication and Enhancement of Immune Functions by the Acyclic Nucleoside Phosphonate 9-(2-Phosphonyl-Methoxyethyl)Adenine (PMEA)
9-(2-phosphonyl-methoxyethyl)adenine (PMEA) is an acyclic nucleoside phosphonate analogue with potent activity against DNA viruses (i.e. herpesviruses) and retroviruses, including human immunodeficiency virus ...
-
Article
Metabolism of anti-herpes agent 5-(2-chloroethyl)-2′-deoxyuridine in mice and rats
The enzymatic splitting and metabolic elimination of anti-viral agent 5-(2-chloroethyl)-2′-deoxyuridine [CEDU] have been studied. For elucidation of structures of metabolites, several different kinds of extrac...
-
Book
-
Chapter
Modes of action of interferon and analogues of 2-5A, a mediator of interferon action
In the last few years, several different interferons have been described, cloned, sequenced, expressed in heterologous systems and purified to homogeneity (Weissmann et al., 1982; Kingsman & Kingsman, 1983). In p...
-
Chapter
Interferon Induction by Nucleic Acids: Structure-Activity Relationships
The first report of a nucleic acid as an interferon inducer was that of Isaacs et al. (1963) who suggested that “foreign” nucleic acids, i.e., those heterologous to the cell in question, were interferon inducers....
