The synthesis, elemental and spectrometric analysis of isoniazid conjugates with polyethylene glycol) (PEG) were obtained. In the first part of the work, acyl isoniazid, hydroxymethyl isoniazid, and modified poly(ethylene glycol) were synthesized. These compounds were characterized by FTIR, by elemental analysis, and by NMR. To obtain antituberculosis macromolecular prodrugs with sustained delivery, the modified PEG were used as carriers by linking, via end group, either isoniazid or its hydroxymethyl derivative.
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References
1.
1. A. Kochi, B. Vareldzis, K. Styblo, Res. Microbiol., 144, (1993), 104.
2.
2. A. J. Domb, S. Amselem, M. Maniar, Biodegradable polymers as drug carrier systems. In: S. Dumitriu, Ed. Polymeric biomaterials, New York, Marcel Dekker, (1994), 399.
3.
3. A. S. Hoffman, Chin. J. Polym. Sci., 13, (1995), 195.
4.
4. B. G. Soares, N. A. De Souza, D. X. Pires, Química Orgânica: teoria e técnicas de preparação e identificação de compostos orgânicos, Rio de Janeiro, Ed. Guanabara, (1988).
5.
5. B. R. Bloom, J. L. Murray, Science, 257, (1992), 1055.
6.
6. C. Perronne, Res. Microbiol., 144, (1993), 129.
7.
7. D. Putnam, J. Kopecek, Adv. Polym. Sci., 122, (1995), 55.
8.
8. D. A. Mitchison, J. Antimicrob. Chemother., 29, (1992), 477.
9.
9. H. Paulsen, D. Stoye, The chemistry of hydrazides. In S. Patai, Ed. The chemistry of amino group, London, Interscience Publishers, (1968), 515.
10.
10. J. E. McGowan, Jr., Res. Microbiol., 144, (1993), 122.
11.
11. J. M. Harris, E. C. Struck, M. C. Case, M. S. Paley, M. Yalpani, J. M. Alstine, D. E. Brooks, J. Appl. Polym. Sci., Polym. Chem. Ed., 22, (1984), 341.
12.
12. J. M. Harris, J. Macromol. Sci.: Rev. Macromol. Chem. Phys., C25, (1985), 325.
13.
13. N. Rastogi, H. L. David, Res. Microbiol., 144, (1993), 133.
14.
14. N. L. Burnham, Am. J. Hosp. Pharm., 51 (1994), 210.
15.
15. P. Krogsgaard-Larsen, H. Bundgaard, Eds., A textbook of drug design and development, Switzerland, Harwood Academic, (1991).
16.
16. R. B. Greenwald, A. Pendri, D. Bolikal, C. W. Gilbert, Bioorg. Med. Chem. Lett., 4, (1994), 2465.
17.
17. S. Dumitriu, M. Dumitriu, Polymeric drug carriers. In: S. Dumitriu, Ed. Polymeric biomaterials, New York, Marcel Dekker, (1994), 435.
18.
18. S. Zalipsky, C. Gilon, A. Zilkha, Eur. Polym. J., 19, (1983), 1117.
19.
19. T. Hayashi, Prog. Polym. Sci., 19, (1994), 663.
20.
20. T. Ouchi, H. Kuroda, K. Hirai, Y. Ohya, J. Macromol. Sci.: Macromol. Reports, A31, (1994), 1091.
21.
21. T. Ouchi, Y. Ohya, Prog. Polym. Sci., 20, (1995), 211.
22.
22. W. R. Jarvis, Res. Microbiol, 144, (1993), 117.
23.
23. Y. Inada, M. Furukawa, H. Sasaki, Y. Kodera, M. Hiroto, H. Nishimura, A. Matsushima, Trends Biotechnol., 13 (1995), 86.
24.
24. Z. Young, A. J. Mesiano, S. Venkatasubramanian, S. H. Gross, J. M. Harris, A. J. Russell, J. Am. Chem. Soc., 117, (1995), 4843.