Design and Synthesis of Organophosphorus Compounds with Antiviral and Other Bioactivities

Autor:	P. Pham, Yung-Chi Cheng, Charles E. McKenna, M. C. Starnes, T. Wen, T.-G. Ye, J.-P. Bongartz, J. N. Levy
Rok vydání:	1990
Předmět:	Viral nucleic acid biology DNA polymerase Chemistry Organic Chemistry Phosphonoacetic Acid Biochemistry Reverse transcriptase Inorganic Chemistry Membrane biology.protein Pi Cotransporter Polymerase
Zdroj:	Phosphorus, Sulfur, and Silicon and the Related Elements. :183-186
ISSN:	1563-5325 1042-6507
DOI:	10.1080/10426509008038936
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
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