Phosphate ester prodrug
Weborganophosphate. [ or″gah-no-fos´fāt] an organic ester of a phosphate such as phosphoric acid with an organic compound such as glucose or sorbitol; see also organophosphorus. … WebPhosphate ester prodrugs substantially enhance the aqueous solubility of some poorly soluble parent drugs due to ionization of the phosphate group at physiological pH. While phosphate prodrugs have proven successful in parenteral formulations, few oral phosphate prodrugs have been marketed to date as they have generally failed to improve parent ...
Phosphate ester prodrug
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WebJun 28, 2008 · A series of amino acid monoester prodrugs of floxuridine was synthesized and evaluated for the improvement of oral bioavailability and the feasibility of target drug delivery via oligopeptide transporters. All floxuridine 5′-amino acid monoester prodrugs exhibited PEPT1 affinity, with inhibition coefficients of Gly-Sar uptake (IC50) ranging from … WebOseltamivir phosphate is an ethyl ester prodrug requiring ester hydrolysis for conversion to the active form, oseltamivir carboxylate. ... In 2-year carcinogenicity studies in mice and rats given daily oral doses of the prodrug oseltamivir phosphate up to 400 mg/kg and 500 mg/kg, respectively, the prodrug and the active form oseltamivir ...
WebNov 13, 2014 · An early focus was pivaloyloxymethyl (POM) modified phosphonates, a prodrug format which was first advanced for use with phosphate monoesters [ 50, 51 ]. However, this approach was readily adapted to phosphonates such as foscarnet esters ( 20) [ 52] and a phosphonate inhibitor of insulin receptor tyrosine kinase [ 53 ]. Web3. Phosphate Esters as Prodrugs of Hydroxyl or Amine Functionalities Phosphate ester prodrugs are typically designed for hydroxyl and amine functionalities of poorly water-soluble drugs with an aim to enhance their aqueous solubility to allow a more favorable oral or parenteral administration (see examples in Table 2).
WebApr 27, 2024 · Fospropofol (Lusedra) is a phosphonooxymethyl prodrug of the sedative or hypnotic drug propofol in which the phosphate promoiety is linked to the sterically … WebApr 12, 2024 · Organophosphorus compounds have found widespread applications in pharmaceuticals, agrochemicals, and materials science. Phosphonates, in particular, can be regarded as isosteres of the corresponding phosphate esters and serve as phosphate mimics in biochemical investigations. 1 The introduction of a phosphonic acid of suitable …
WebMay 1, 2001 · Fosphenytoin is a phosphate ester prodrug of phenytoin with an improved solubility and better tolerance after intramuscular or intravenous administration. It is rapidly hydrolyzed in vivo to phenytoin with a half-life of 5–15 min. The prodrug is not pharmacologically active, but it has been shown to cross-react in various immunoassays …
WebNov 15, 2024 · These eight prodrugs are aripiprazole lauroxil, isavuconazonium sulfate, ixazomib citrate, sacubitril, selexipag, tenofovir alafenamide sulfate, uridine triacetate, and telotristat etiprate with their respective metabolites aripiprazole, isavuconazole, ixazomib, LBQ657, ACT-333679, tenofovir, uridine, and telotristat being pharmacologically … china buffet menu mason city iaWebMay 23, 2016 · Phosphate Esters In drug design, forming phosphate esters is a common strategy making the drug more soluble in water. In addition to good water solubility, the phosphate ester can also be a site of the substrate for alkaline phosphatases, this property enables the paclitaxel prodrug to have a fast release of the parent drug. grafico mixed in keyWebNov 11, 2024 · Main protease (M pro) is a superior target for anti-SARS-COV-2 drugs. PF-07304814 is a phosphate ester prodrug of PF-00835231 that is rapidly metabolized into the active metabolite PF-00835231 by alkaline phosphatase (ALP) and then suppresses SARS-CoV-2 replication by inhibiting M pro. china buffet mentor on the lakeWebPhosphate ester prodrugs are typically designed for hydroxyl and amine functionalities of poorly water-soluble drugs with an aim to enhance their aqueous solubility to allow a … grafico in wordWebtriphenylethylene phosphate prodrug, TAT-59, were also conducted in the rat intestinal perfusion model. Finally, the utility of a phosphate ester prodrug strategy for entacapone to increase that drugs systemic levels was evaluated in rats. MATERIALS AND METHODS Materials TAT-59 and its parent drug, DP-TAT-59, were gifts of china buffet menu houghotn lakeWebJan 1, 2024 · Phosphate ester group. Phosphate esters are the most commonly used for prodrug synthesis to increase the solubility of poorly water-soluble orally administered drugs as well as for drugs that are administered parenterally (Stella and Nti-Addae, 2007). The phosphate prodrug is acted upon by endogenous phosphatase enzymes like alkaline ... china buffet menu frankfortWebPhosphate ester prodrugs of propofol (fospropofol, HX0969W) were designed to avoid the unsatisfactory water solubility of the parent drug. However, in previous clinical trials, there … china buffet menu union city tn