20464-68-0Relevant academic research and scientific papers
Synthesis and biological evaluation of aryl phosphoramidate prodrugs of fosfoxacin and its derivatives
Munier, Mathilde,Tritsch, Denis,Lièvremont, Didier,Rohmer, Michel,Grosdemange-Billiard, Catherine
, (2019/06/08)
Aryl phosphoramidate prodrugs of fosfoxacin derivatives 15a-b and 8a-b were synthesized and investigated for their ability to target bacteria. No growth inhibition was observed neither for Mycobacterium smegmatis nor for Escherichia coli on solid medium,
PHOSPHORAMIDATES OF MONOSACCHARIDES
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Page/Page column 29, (2012/08/27)
The present invention relates novel phosphorainidates of monosaccharides of formula (I), wherein R1 is a monosaccharide group selected from A and B: R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16 and X are as defined herein. Preferably X is -0-. The present invention also provides processes for the production of compounds of formula (I), pharmaceutical compositions comprising these compounds, as well as to the use thereof in medical therapy, preferably in the treatment of osteoarthritis. Formula (I) wherein: R1 is selected from A and B.
Novel phosphoramidate prodrugs of N-acetyl-(d)-glucosamine with antidegenerative activity on bovine and human cartilage explants
Serpi, Michaela,Bibbo, Rita,Rat, Stephanie,Roberts, Helen,Hughes, Claire,Caterson, Bruce,Alcaraz, María José,Gibert, Anna Torrent,Verson, Carlos Raul Alaez,McGuigan, Christopher
supporting information; experimental part, p. 4629 - 4639 (2012/07/01)
(d)-Glucosamine and other nutritional supplements have emerged as safe alternative therapies for osteoarthritis (OA), a chronic and degenerative articular joint disease. In our preceding paper, a series of novel O-6 phosphate N-acetyl (d)-glucosamine prod
Phosphoramidates of monosaccharides
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Page/Page column 18-19, (2012/07/14)
The present invention relates novel phosphoramidates of monosaccharides of formula (I), wherein R1 is a monosaccharide group selected from A and B; R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16 and X are as defined herein. Preferably X is -O-. The present invention also provides processes for the production of compounds of formula (I), pharmaceutical compositions comprising these compounds, as well as to the use thereof in medical therapy, preferably in the treatment of osteoarthritis. wherein: R1 is selected from A and B,
Aryl phosphoramidates of 5-phospho erythronohydroxamic acid, a new class of potent trypanocidal compounds
Ruda, Gian Filippo,Wong, Pui Ee,Alibu, Vincent P.,Norval, Suzanne,Read, Kevin D.,Barrett, Michael P.,Gilbert, Ian H.
supporting information; experimental part, p. 6071 - 6078 (2010/11/16)
RNAi and enzymatic studies have shown the importance of 6-phosphogluconate dehydrogenase (6-PGDH) in Trypanosoma brucei for the parasite survival and make it an attractive drug target for the development of new treatments against human African trypanosomi
Phosphate prodrugs derived from N-acetylglucosamine have enhanced chondroprotective activity in explant cultures and represent a new lead in antiosteoarthritis drug discovery
McGuigan, Christopher,Serpi, Michaela,Bibbo, Rita,Roberts, Helen,Hughes, Clare,Caterson, Bruce,Gibert, Ana Torrent,Verson, Carlos Raúl Alaez
experimental part, p. 5807 - 5812 (2009/09/06)
We report the application of the phosphoramidate ProTide approach, developed by us for antiviral nucleosides, to sugar derivatives with potential chondroprotection against osteoarthritis. In particular, N-acetylglucosamine was converted to a series of 06
Antiviral phosphoramidates
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Page/Page column 41, (2008/06/13)
The invention provides novel nucleoside compounds of formula I wherein R1, R2a, R2b, R3, R4, R5, R6, R8a, R9 and R10 are as defined herein which are useful for the treatment of Hepatitis C Virus (HCV) mediated diseases. The invention further provides methods for treatment or prophylaxis of HCV mediated diseases with compounds of formula I and pharmaceutical compositions comprising these compounds,
Cytotoxic nucleoside analog compound 003 for treating cancer
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Page/Page column 6; 14-15, (2008/06/13)
The present invention provides pharmaceutical compositions comprising Compound 003 or metabolites thereof in combination with one or more carboxylesterase inhibitors. The invention provides methods for inhibiting cellular proliferation associated with pro
PHOSPHORAMIDATE DERIVATIVES
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Page/Page column 25, (2008/06/13)
The present invention provides a phosphoramidate compound comprising the structure (I) Formula (I)wherein: X comprises a monosaccharide group comprising the structure (II) or (III),8Formula (II) , (III) B and B are independently selected from the group co
Anti-proliferative and anti-leukemic activity of DDE46 (compound WHI-07), a novel bromomethoxylated arylphosphate derivative of zidovudine, and related compounds: Studies using human acute lymphoblastic leukemia cells and the zebrafish model
Benyumov, Alexey O.,Venkatachalam, Taracad K.,Grigoriants, Olga O.,Vassilev, Alexei O.,Tibbles, Heather E.,Downs, Suzanne,Dumez, Darin,Uckun, Fatih M.
, p. 114 - 122 (2007/10/03)
The anti-proliferative effects of a novel bromomethoxylated arylphosphate derivative of zidovudine (compound DDE46, CAS 213982-96-8) were first examined in a zebra fish embryo model. DDE46 blocked the cell division at the 2-cell stage of the embryonic development followed by total cell fusion. DDE46 also inhibited the proliferation of the leukemic cell lines NALM-6 and MOLT-3. DDE46 enhanced the activity of the pro-apoptotic enzymes Caspase-3, Caspase-6, Caspase-8, and Caspase-9 leading to the apoptotic death of the leukemic cell line Jurkat. These results justify the further development of this agent as a new anti-leukemic drug candidate. ECV · Editio Cantor Verlag, Aulendorf (Germany).
