Antiviral Action and Cellular Toxicity of Four Thymidine Analogues: 5-Ethyl-, 5-Vinyl-, 5-Propyl-, and 5-Allyl-2′-Deoxyuridine
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چکیده
منابع مشابه
Evaluation of (5R,6R)-5-Bromo-6-Ethoxy-5-Ethyl-5,6-Dihydro-2\'- Deoxyuridine as a Brain-Targeted Prodrug of 5-Ethyl-2\'- Deoxyuridine
(+)-Trans-(5R,6R)-5-bromo-6-ethoxy-5-ethyl-5,6-dihydro-2'-deoxyuridine [(5R,6R)-BEEDU], a potential brain-targeted prodrug of 5-ethyl-2'-deoxyuridine (EDU), was synthesized by the regiospecific addition of BrOEt to the 5,6-olefinic bond of EDU. (5R,6R)-BEEDU is more lipophilic (log P = 0.04) than EDU (log P = -1.09). In vitro incubation of (5R,6R)-BEEDU with rat whole blood and brain homogena...
متن کاملSynthesis of 5-substituted 2'-deoxyuridine-5'- phosphonate analogues and evaluation of their antiviral activity.
A small series of 5-(hetero)aryl-modified nucleoside phosphonates was synthesized via an 8-step procedure including a Wittig reaction and Suzuki-Miyaura coupling. An unanticipated anomerization during phosphonate deprotection allowed us to isolate both anomers of the 5-substituted 2'-deoxy-uridine phosphonates and assess their antiviral activity against a broad panel of viruses.
متن کاملevaluation of (5r,6r)-5-bromo-6-ethoxy-5-ethyl-5,6-dihydro-2'- deoxyuridine as a brain-targeted prodrug of 5-ethyl-2'- deoxyuridine
(+)-trans-(5r,6r)-5-bromo-6-ethoxy-5-ethyl-5,6-dihydro-2'-deoxyuridine [(5r,6r)-beedu], a po tential brain-targeted prodrug of 5-ethyl-2'-deoxyuridine (edu), was synthesized by the regiospecific addition of broet to the 5,6-olefinic bond of edu. (5r,6r)-beedu is more lipophilic (log p = 0.04) than edu (log p = -1.09). in vitro incubation of (5r,6r)-beedu with rat whole blood and brain...
متن کامل5-Propyl-2'-deoxyuridine: a specific anti-herpes agent.
In both primary rabbit kidney cells and human skin fibroblasts, 5-propyl-2'-deoxyuridine proved inhibitory to herpes simplex virus at a concentration as low as 1 micrograms/ml, whereas concentrations higher than 200 micrograms/ml were required to inhibit vaccinia virus replication or normal cell metabolism.
متن کاملEvaluation of (5R,6R)-5-Bromo-6-Ethoxy-5-Ethyl-5,6-Dihydro-2'- Deoxyuridine as a Brain-Targeted Prodrug of 5-Ethyl-2'- Deoxyuridine
(+)-Trans-(5R,6R)-5-bromo-6-ethoxy-5-ethyl-5,6-dihydro-2'-deoxyuridine [(5R,6R)-BEEDU], a potential brain-targeted prodrug of 5-ethyl-2'-deoxyuridine (EDU), was synthesized by the regiospecific addition of BrOEt to the 5,6-olefinic bond of EDU. (5R,6R)-BEEDU is more lipophilic (log P = 0.04) than EDU (log P = -1.09). In vitro incubation of (5R,6R)-BEEDU with rat whole blood and brain homogenate...
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ژورنال
عنوان ژورنال: Antimicrobial Agents and Chemotherapy
سال: 1976
ISSN: 0066-4804,1098-6596
DOI: 10.1128/aac.10.1.119