Prodrugs synthesis

H. Bundgaard, N. M. Nielsen, A. Buur, Aspirin Prodrugs Synthesis and Hydrolysis of 2-Acetoxybenzoate Esters of Various V-(Hydroxyalkyl)amides , Int. J. Pharm. 1988, 44, 151-158. 

F. A. Omar, Cyclic Amide Derivatives as Potential Prodrugs. Synthesis and Evaluation of V-Hydroxymethylphthalimide Esters of Some Non-Steroidal Anti-Inflammatory Car-boxy he Acid Drugs , Eur. J. Med. Chem. 1998, 33, 123-131. 

R. Niemi, J. Vepsalainen, H. Taipale, T. Jarvinen, Bisphosphonate Prodrugs Synthesis and in vitro Evaluation of Novel Acyloxyalkyl Esters of Clodronic Acid , J. Med. Chem. 1999,42, 5053-5058. 

Merk, N., H. Bundgaard, M. Shalmi, and S. Christensen. 1990. Furosemide prodrugs synthesis, enzymatic hydrolysis and solubility of various furosemide estirt. J. Pharm.60 163-169. 

It is also clear from the data presented in this chapter that care must be taken when applying any of the above-proposed solutions. Logical selection of excipients and rational design of lipid-based formulations or prodrug synthesis tailored for drug candidates are key factors for the success of these delivery systems. 

Ahlmark, M., Vepsaelaeinen, J., Taipale, H., Niemi, R., Jaervinen, T. Bisphophonate prodrugs synthesis and in vitro evaluation of novel clodronic acid dianhydrides as bioreversible prodrugs of clodronate. J. Med. Chem. 1999,42,1473-1476. 

Bundgaard, H., Falch, E., Larsen, C., Mikkelson, T. J. Pilocarpine prodrugs Synthesis, stability, bioconversion, and physicochemical properties of sequentially labile pilocarpine acid diesters. J. Pharm. Sci. 1986, 75, 36-44. 

Turhanen, P.A., Ahlgren, M.J., Jarvinen, T., and Vepsalainen, J.J., Bisphosphonate prodrugs. Synthesis and identification of (1-hydroxyethylidene)-1,1-bisphosphonic acid tetraesters by mass spectrometry, NMR spectroscopy and X-ray crystallography. Phosphorus, Sulfur Silicon Relat. Elem., 170, 115, 2001. Pudovik, A.N., Batyeva, E.S., and Zamaletdinova, G.U., Reaction of a trimethylsilyl phosphite with O,O-diethyl acetyIphosphonate, Zh. Obshch. Khim., 43, 680, 1973 J. Gen. Chem. USSR (Engl. Transl.), 43, 676, 1973. 

Angewandte Makromolelmlare Chentie Vol.245, March 1997, p.1-8 POLYMERIC PRODRUGS SYNTHESIS, RELEASE STUDY AND ANTIMICROBIAL PROPERTIES OF POLYMER-BOUND ACRIFLAVINE... 

The pharmacokinetics of the active moiety should be well documented before starting prodrug synthesis, and, at a later stage, prodrug kinetics should be thoroughly investigated in humans. 

A frequently used technique in the optimization of drug delivery, regardless of the route selected, has been prodrug synthesis. In this approach, a drug is chemically modified to optimize its delivery properties. Normally, this means increasing either... 

Niemi R, Vepsalainen J, Taipale H, Jarvinen T (1999) Bisphosphonate prodrugs synthesis and in vitro evaluation of novel acyloxyalkyl esters of clodronic acid. J Med Chem 42 5053-5058... 

Monteil M, Migianu-Giiffoni E, Sainte-Catherine O, Di Benedetto M, Lecouvey M (2014) Bisphosphonate prodrugs synthesis and biological evaluation in HuH7 hepatocarcinoma cells. Eur J Med Chem 77 56-64... 

Another prodrug synthesis using a microfluidic reaction system is that of the antibiotic ciprofloxacin [10], A microreaction system developed by CPC systems (CYTOS) was used as a reaction apparatus. This system is the size of a videotape with a holdup of 1.8 ml. The high surface-to-volume ratio for the mixing section as well as for the temperature-controlled reaction channels allows heat transfer coefficients of up to 2,000 Wm K . The synthesis has demonstrated the potential for faster development, particularly in the preparation of relevant quantities for development studies, such as clinical trials, using the microreaction systems. 

H. Patel, D. A. Raval, D. Madamwara, and S.R. Patel, Polymeric prodrug Synthesis, release study and antimicrobial property of poly(styrene-co-maleic anhydride)-bound acriflavine, DieAngew. Makromol. Chem., 263 (1), 25-30,1998. 

Adler, C.A., Maurice, D.M. and Paterson, M.E., 1971, The effect of viscosity of the vehicle on the penetration of fluorescein into the human eye. Exptl. Eye Res. 11 34 Blaug, S.M. and Canada, A.T., 1965, Relationship of viscosity, contact time and prolongation of action of methylcellulose-containing ophthalmic solutions. Amer. J. Hosp. Pharm., 22 662 Bungaard, H., Buur, A., Chang, S-C. and Lee, V.H.L., 1988, Timolol prodrugs synthesis, stability and lipophilicity of various alkyl, cycloalkyl and aromatic esters of timolol. Int J. Pharm., 46 77 Chrai, S.S. and Robinson, J.R., 1974, Ocular evaluation of methylcellulose vehicle in albino rabbits. 

Zhou L, Cheng R, Tao H, Ma S, Guo W, Meng F. Endosomal pH-activatable poly(ethylene oxide)-graft-doxorubicin prodrugs synthesis, drug release, and biodistribution in tumor-bearing mice. Biomacromolecules 2011 12 1460-7. 

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