Synthesis and applications of phosphonoacetic derivatives.
In this paper, the synthesis of new phosphonoacetic acid derivatives and their applications in fields of biotechnological interest are discussed. Phosphonoacetic acids are competitive inhibitors of alkaline phosphatase, an enzyme widely used in diagnostics, as colorimetric detection tool. The phosphonoacetic acid's inhibition activity has been exploited by us for the obtainment of an innovative technique for non-radioactive DNA probes detection, the last being based on DNA labeling with the enzyme inhibitor, followed by detection by means of the chromogenic enzyme and substrate. Moreover, we have found a further application of phosphonoacetic acids, by the preparation of an affinity chromatography support that has been revealed to be very effective in the purification of alkaline phosphatase. Finally, phosphonoacetic acid derivatives have been tested also for their antiviral activity. Some of them, examined in preliminary in vitro experiments, have been found very active against Herpes simplex virus.
Davini
E
E
Eniricerche SpA, Monterotondo Scalo, Italy.
Di Leo
C
C
Norelli
F
F
Zappelli
P
P
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002846:Chromatography, Affinity; D004247:DNA / Q000032:analysis; D015342:DNA Probes; D007700:Kinetics; D015394:Molecular Structure; D010746:Phosphonoacetic Acid / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D018139:Simplexvirus / Q000187:drug effects
D000998:Antiviral Agents; D015342:DNA Probes; D004247:DNA; D010746:Phosphonoacetic Acid