| Autor: |
T.-G. Ye, M. C. Starnes, P. Pham, Yung-Chi Cheng, Charles E. McKenna, T. Wen, J. N. Levy, J.-P. Bongartz |
| Rok vydání: |
1990 |
| Předmět: |
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| Zdroj: |
ChemInform. 21 |
| ISSN: |
0931-7597 |
| DOI: |
10.1002/chin.199045355 |
| Popis: |
Investigations of phosphonates and related biophosphate analogues as inhibitors of viral nucleic acid polymerases are summarized. General syntheses of α-halo phosphonoacetic acid (PAA) and methanediphosphonic acid (MDP) derivatives have been extended to preparation of seven α-halo phenyl (phosphonomethyl) phosphinates (PhMpP). Two phosphonates containing potentially reactive α-keto groups, oxophosphonoacetate (phosphonoglyoxalate, COPAA) and oxomethanediphosphonate (carbonyldiphosphonate, COMDP) are discussed. A convenient, two-step synthesis of trisodium thiophosphonoformate (TPFA) from trimethyl phosphonoformate (Me3PFA) [via Me3TPFA) is presented. TPFA selectively inhibits HIV-1 reverse transcriptase (RT) relative to both human DNA polymerase α (pol α) and four herpesvirus DNA polymerases. The significance of membrane Na+/Pi cotransport inhibition by phosphonates is briefly addressed. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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