131853-06-0Relevant articles and documents
Synthesis of oxime nerve agent antidotes
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Page/Page column 6; 7, (2020/05/16)
The present invention relates to a new route to bis-quaternary pyridinium oximes which can be utilized to restore activity of acetylcholinesterase inhibited by combination with organophosphates.
Nucleoside analogs
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, (2008/06/13)
Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula STR1 wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl and B is a purine or pyrimidine base. A compound of formula (VI) STR2 wherein X is halogen, Y is S-phenyl, Se-phenyl or halogen and B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, 2-acetamido-6-diphenylcarbamoylpurine, 6-N-dimethylamino-methyladenine or 6-N-pivaloyladenine. A compound of formula (VII) STR3 wherein B is guanine, 8-guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, or 5-methylcytosine.
A New Class of Acyclic Phosphonate Nucleotide Analogues: Phosphonate Isosteres of Acyclovir and Ganciclovir Monophosphates as Antiviral Agents
Kim, Choung Un,Misco, Peter F.,Luh, Bing Yu,Hitchcock, Michael J. M.,Ghazzouli, Ismail,Martin, John C.
, p. 2286 - 2294 (2007/10/02)
Novel pohosphonate isosteres of acyclovir (ACV) and ganciclovir (DHPG) monophosphates (20 and 32) wre foudnd to be potent and selective antiherpesvirus agents.In the series of phosphonate analogues of ACV monophosphate, only the guanine analogue 20 exhibited activity against herpesviruses, similar to the structure-activity relationship observed for base modification of ACV analogues.The phosphonate isostere of ACV monophosphate (20) was more effective than ACV in the HSV-1 infected mouse model.The 3'-carba analogues of 9-purines/pyrimidines (adenine, HPMPA; guanine, HPMPG; cytosine, HPMPC) are devoid of antiherpesvirus activity.This result confirms that the β-oxygen atom of the phosphonomethyl ether functionality in HPMP-purines/pyrimidines plays a critical role for activity against herpesviruses.
SYNTHESIS OF A PHOSPHONATE ISOSTERE OF ACYCLOVIR MONOPHOSPHATE: A HERPESVIRUS ACTIVE PHOSPHONATE NUCLEOTIDE ANALOGUE
Kim, Choung Un,Misco, Peter F.,Luh, Bing Y.,Martin, John C.
, p. 1571 - 1574 (2007/10/02)
A novel synthetic methodology for the acyclic acetal functionality was developed.The rationally designed phosphonate analogue (3) of acyclovir monophosphate was active against herpesviruses.