Brazilian Chemical Society (SBQ). Division of Medicinal Chemistry. 4th Brazilian Symposium on Medicinal Chemistry
Synthesis of prodrug with therapeutic potential for tuberculosis

meningitis using CDS
Pinto, L.S.R.1; Fernandes, J.T. 2; Regasini3, L.O.; Peccinini, R.G.1; Silva, M.2*; [email protected]
Depto de Princípios Ativos Naturais e Toxicologia - Faculdade de Ciências Farmacêuticas - UNESP - Rod. Araraquara
- Jaú Km 01, CEP.14801-902 - Araraquara-SP – Brasil
2Lapdesf – Lab. de Pesquisa e Desenvolvimento de Fármacos - Depto de Fármacos e Medicamentos - Faculdade de
Ciências Farmacêuticas - UNESP - Rod. Araraquara - Jaú Km 01, CEP.14801-902 - Araraquara-SP – Brasil
3Instituto de Química - UNESP – Prof. Francisco Degni, CEP.14801-970 - Araraquara-SP – Brasil

Keywords: prodrug, CDS, ethambutol.
from samples in KBr pellets with a Shimadzu Introduction
spectrophotometer. 13C and 1H spectra were collected in the Advance DPX300 spectrometer The inefficiency of many drugs in the brain sickness (Brüker) at 500 MHz, using 5 mm diameter treatment results of the incapability to transport the resonance tubes, with CDCl3, DMSO-d6. Melting- blood-brain barrier (BBB) and maintain adequate ranges of products were measured, without levels of concentrations in the central nervous correction, in an Electrothermal melting-point system (CNS)1,2. Chemical approaches to improve apparatus. Analytical thin-layer chromatography was brain uptake of a therapeutic agent rely on molecular used to monitor the purification of synthesized First, a CDS should be sufficiently lipophilic to enter pharmacologically active species to improve the the central compartment. The molecule should then deficient physicochemical properties. In designing a undergo to an enzymatic and/or chemical conversion chemical delivery systems (CDS)3-5 for the CNS, the to promote retention in the CNS. It is expected that, unique architecture of the BBB can actually be at the same time, peripheral elimination of the entity is accelerated due to facile conversion of the CDS in the body. Results and Discussion
In this work, to obtain a redox CDS and improve the Conclusions
access of tuberculostatic agent to the CNS for tuberculosis meningitis treatment, ethambutol was The present study was intended to contribute to the development of new anti-tuberculosis drug using intermediate was then quaternized to generate the CDS. The CDS approach may offer many promising pyridinium salts and the ethambutol prodrug The possibilities for brain delivery and targeting, like the reactions involved in the synthesis of the ethambutol increase brain concentrations of ethambutol and the Acknowledgements
Authors would like to thank the Fapesp and FCFAr- Thwaites, G. E.; Hien, T. T. Lancet Neurol., 2005,4,160.
Katti, M. K. Med. Sci. Monit., 2004, 10,215.
3Bodor, N.; Buchwald, P. Am. J. Drug Delivery, 2003, 1,13.
4Yoon, S.H., Wu, J., Bodor N. Bull. Korean Chem. Soc., 2002, 23, 761.
Bodor, N., Farag, H. H. J. Med. Chem., 1983, 26, 528.
(ethambutol prodrug) (pyridinium ethambutol salt) Figure 1. Synthesis of ethambutol prodrug.
(EBM - ethambutol, NA - nicotinic acid, NEB -

The compounds were structurally characterized and identified: infrared absorption spectra in the wavelengths range 4000 to 400 cm-1 were obtained 4th Brazilian Symposium on Medicinal Chemistry – BrazMedChem2008

Source: http://www.iqsc.usp.br/brazmedchem/CD/resumos/02/R0446-1.pdf


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