• Latanoprost is administered in the isopropyl ester form shown here, which is then hydrolysed in vivo in to active metabolite lanoprost free acid. (guidetopharmacology.org)
  • Latanoprost, an isopropyl ester prodrug, is a prostaglandin F 2α analogue and a selective prostanoid agonist. (mims.com)
  • Across a chain length range of 6 to 12 carbon atoms, a length of 9 or 10 carbon atoms (nonanoate or decanoate ester) was found to be optimal in rodents in the case of testosterone esters. (wikipedia.org)
  • The presentation of longer-acting testosterone esters like testosterone enanthate, testosterone cypionate, and testosterone undecanoate beginning during the 1950s brought about testosterone propionate for the most part being superseded. (etalaze.biz)
  • Six ketoprofen (CAS 22071-15-4) atkylazacycloalkan-2-one ester derivatives (I-VI) were synthesized and evaluated for their anti-inflammatory, analgesic, and ulcerogenic activities after oral administration. (unict.it)
  • The amino acid ester derivatives of 6-deoxypenciclovir, 11-20, were synthesized as potential prodrugs of penciclovir, and were evaluated for their oral penciclovir bioavailability in mice and rats. (ewha.ac.kr)
  • using conventional coupling method (DCC/DMAP) afforded the mono-O-ester derivatives 1-5 in 47-55% yields as a mixture of two diastereomers along with the di-O-ester derivatives 6-10 in 20-29% yields. (ewha.ac.kr)
  • Reductive cleavage of carbobenzyloxy (Cbz) group (10% Pd/C, 1 atmosphere of H 2 , room temperature in methanol) followed by subsequent treatment of the resulting free amine with methanolic HCl solution provided the mono-O-ester derivatives 11-15 as di-HCl salt in 51-98% yields and the di-O-ester derivatives 16-20 as tri-HCl salt in 65-98% yields. (ewha.ac.kr)
  • Prodrugs are derivatives of drug molecules that are pharmacologically inactive but require either chemical or enzymatic transformation to release the active drug in vivo in order to exert a pharmacological effect. (ijpsonline.com)
  • The optically enriched β-cyano carboxylic esters from our method can be readily transformed to medicines that include γ-aminobutyric acids derivatives such as Rolipram. (stanford.edu)
  • A convenient and simple way to synthesize polymerizable ribavirin derivatives is via transesterification between ribavirin and divinyl dicarboxylates in acetone at 50 ºC, catalyzed by lipase immobilized on acrylic resin from Candida antarctica (CAL-B). These ribavirin esters can be consequently homo-polymerized or copolymerized with other bioactivity compounds such as sugar vinyl esters to form prodrugs which are useful in pharmacy. (news-medical.net)
  • 9~ yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R, 5S, cis)-4-amino-5- fluoro-l-(2~ hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, EmtrivaTM, (-)-cis FTC) and their physiologically functional derivatives. (gc.ca)
  • Related furazan derivatives, aspirin, its propyl ester, and its gamma-nitrooxypropyl ester were taken as references. (uhi.ac.uk)
  • All the products described present an antiinflammatory trend, maximized in derivatives 12, 16, and 17, they are devoid of acute gastrotoxicity, principally due to their ester nature, and show an antiplatelet activity primarily determined by their ability to release NO. They do not behave as aspirin prodrugs in human serum. (uhi.ac.uk)
  • Though several studies have been carried out on various prodrugs, surprisingly very few reviews on different carriers, which can be used for prodrug synthesis were published to date. (ijpsonline.com)
  • In this review different types of carriers, which can be used for prodrug synthesis are summarized. (ijpsonline.com)
  • The objective of this review is to provide the researchers with a compilation of which carriers would be suitable for prodrug synthesis and what would be their benefits. (ijpsonline.com)
  • To minimize ribavirin-induced hemolysis and increase its antiviral effect, considerable efforts have been made involving chemical prodrugs and various formulations. (news-medical.net)
  • An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza. (mcw.edu)
  • In this study, physicochemical properties and pH rate profiles of 3 diclofenac ester prodrugs differing with respect to the spacer carbon chain length between the drug and the imidazole-based promoiety were determined and a rate equation for prodrug degradation in aqueous solution in the pH range 1-10 was derived. (ku.dk)
  • Carrier-linked prodrugs are for drugs with major drawbacks, which are linked to a nontoxic carrier or promoiety through covalent linkage to change or get rid of their undesirable physicochemical properties. (ijpsonline.com)
  • Store at room using your blood trenbolone ester prodrugs, including trenbolone acetate (brand names. (awingsoft.com)
  • enanthate ester and a long-acting prodrug of trenbolone. (tophygetropin.com)
  • The prodrug strategy implementation in the last 20 y has led to a steady advancement in the biopharmaceutical, physicochemical and/or pharmacokinetic attributes of the pharmacologically active compounds. (ijpsonline.com)
  • The only difference in the compounds is the ester attached, which helps to control the hormone's releasing activity. (tophygetropin.com)
  • VASOTEC® (Enalapril Maleate) is the maleate salt of enalapril, the ethyl ester of a long-acting angiotensin -converting enzyme inhibitor, enalaprilat. (rxlist.com)
  • following oral administration, it is bioactivated by hydrolysis of the ethyl ester to enalaprilat, which is the active angiotensin-converting enzyme inhibitor. (rxlist.com)
  • A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. (mcw.edu)
  • Certain sulfur-based steroid esters have a sulfamate or sulfonamide moiety as the ester, typically at the C3 and/or C17β positions. (wikipedia.org)
  • These prodrugs subsequently undergo enzymatic or non-enzymatic cleavage to release the active drug moiety (figure 1) [ 12 , 13 ]. (ijpsonline.com)
  • The oral formulations of all veterinary ACE inhibitors (benazepril, enalapril, imidapril and ramipril) correspond to the pro-drug, i.e., an ester of the active moiety, which is absorbed from the digestive tract. (vin.com)
  • An inactive or weakly active substance that has an active metabolite is called a prodrug, especially if designed to deliver the active moiety more effectively. (msdmanuals.com)
  • A prodrug approach for local and sustained diclofenac action after injection into joints based on ester prodrugs having a pH-dependent solubility is presented. (ku.dk)
  • Inherent ester prodrug properties influencing the duration of action include their pH-dependent solubility and charge state, as well as susceptibility to undergo esterase facilitated hydrolysis. (ku.dk)
  • Esterification is useful because it is often able to render the parent steroid into a prodrug of itself with altered chemical properties such as improved metabolic stability, water solubility, and/or lipophilicity. (wikipedia.org)
  • The greater solubility in oil allows the steroid esters to be dissolved in a smaller oil volume, thereby allowing for larger doses with intramuscular injection. (wikipedia.org)
  • The prodrug degradation was found to be about 6-fold faster in 80% (vol/vol) human plasma as compared to 80% (vol/vol) human synovial fluid with 2-(1-methyl-1H-imidazol-2-yl)ethyl 2-(2-(2,6 dichlorophenyl)amino)phenylacetate being the poorest substrate toward enzymatic cleavage. (ku.dk)
  • The conversion and release of parent diclofenac from prodrug suspensions in vitro were studied using the rotating dialysis model. (ku.dk)
  • Fatty acid esters increase the lipophilicity of steroids, with longer fatty acids resulting in greater lipophilicity. (wikipedia.org)
  • The results suggest that it is possible to alter and control dissolution and reconversion behavior of the diclofenac prodrugs, thus making the prodrug approach feasible for local and sustained diclofenac action after joint injection. (ku.dk)
  • The prodrug approach using various carriers has evolved as a significant tool in surmounting different obstacles in relation to drug formulation and targeting. (ijpsonline.com)
  • The prodrug approach is rapidly becoming a crucial part in the stratagem of delivery of drugs. (ijpsonline.com)
  • The success of the prodrug approach can be measured by examining how many prodrugs are currently on the market. (ijpsonline.com)
  • the prodrug approach may be truly selective because it requires the aberrant high ROS levels in cancer cells to activate it. (5dok.net)
  • It is a 3-carboxamidine prodrug of ribavirin, developed to target the liver and subsequently avoid the erythrocyte accumulation (with resulting anemia) often associated with ribavirin therapy. (news-medical.net)
  • In the pH range 6-10, the prodrugs were subject to parallel degradation to yield diclofenac and an indolinone derivative. (ku.dk)
  • Abstract A carbene-catalyzed asymmetric access to chiral β-cyano carboxylic esters is disclosed. (stanford.edu)
  • In the mouse acetic acid induced writhing assay, the prodrugs exhibited, following acute administration, a good analgesic activity. (unict.it)
  • Unlike other steroid esters however, they bypass first-pass metabolism with oral administration and have high oral bioavailability and potency, abolished first-pass hepatic impact, and long elimination half-lives and durations of action. (wikipedia.org)
  • Valopicitabine (oral valine ester prodrug of 2′- C -methylcytidine). (cdc.gov)
  • Dabigatran etexilate is an oral prodrug that is hydrolyzed to the competitive and reversible direct thrombin inhibitor dabigatran . (drugbank.com)
  • NfsB is a dimeric flavoprotein enzyme that has broad electron acceptor specificity 15 and has been used in conjunction with prodrugs to selectively ablate cells in vertebrates. (cdc.gov)
  • Prodrug concept is justified because it enables the active drug to overcome the barrier that would impede it from reaching the site of action to exert the required pharmacological activity. (ijpsonline.com)
  • A bioprecursor prodrug is transformed chemically through hydration (for example, lactones such as some statins), reduction (for example, sulindac, platinum (IV) complexes) or oxidation (for example, dexpanthenol, nabumetone) or metabolically to the active agent [ 5 , 9 - 11 ]. (ijpsonline.com)
  • Dabigatran etexilate is a double prodrug that is hydrolyzed to the active dabigatran by intestinal and hepatic carboxylesterases. (drugbank.com)
  • All the prodrugs showed a good stability both in pH 7.4 phosphate buffer and in pH 2.0 buffer, and they were readily hydrolyzed by rat plasma. (unict.it)
  • Examples include cortisone acetate and hydrocortisone and its esters. (wikipedia.org)
  • Examples of both marketed and investigational prodrugs using several promoieties are discussed with their advantages and future prospects. (ijpsonline.com)
  • Around 10 % of marketed medicines can be categorized as prodrugs currently, and also that during 2008, 33 % of approved small molecular weight drugs were prodrugs [ 5 - 7 ]. (ijpsonline.com)
  • Clinical data for TP, Tempol Hydroxylamine (TP-H), and the more lipophilic TP-H prodrug, OT-551, are reviewed. (frontiersin.org)
  • Prodrugs have better delivery properties that surpass the parent drug molecule [ 1 ]. (ijpsonline.com)
  • A new series of NSAIDs in which aspirin is joined by an ester linkage to furoxan moieties, with different ability to release NO, were synthesized and tested for NO-releasing, antiinflammatory, antiaggregatory, and ulcerogenic properties. (uhi.ac.uk)
  • Diphosphate ester salt of phenytoin acts as water-soluble prodrug of phenytoin. (medscape.com)
  • Properties and selection of carriers or promoeities is a very important parameter in successful prodrug design. (ijpsonline.com)
  • Esters I-VI showed an anti-inflammatory activity, determined as the percent of inhibition of carrageenan-induced edema, similar to that of ketoprofen, although at higher doses. (unict.it)
  • which is recommended as control reagent in nucleotide-AM ester applications. (biolog.de)
  • Dr. Liu's research interest is to develop molecularly targeted drug delivery systems, such as nanoparticles, nanoconjugates and prodrugs, to improve tumor specific delivery of small molecule anticancer drugs and biologics (RNAs, peptides, and antibodies) to target cancer metastasis. (uh.edu)
  • It was the primary testosterone ester to be promoted, and was the significant type of testosterone utilized in medication until around 1960. (etalaze.biz)