Latenciacao de quimioterapicos-sintese de acriloilderivados de antimalaricos / Drug latentiation: synthesis of acriloylderivatives of antimalarial agents

Com o objetivo de se obter, atraves do metodo da latenciacao, pro-farmacos de acao antimalarica prolongada e menor toxicidade, foram sintetizados derivados acriloilicos da dapsona e das seguintes sulfas antimalaricas: sulfadiazina, sulfadimetoxina, sulfadoxina, sulfametoxazol, sulfametoxidiazina, sulfametoxipiridazina, sulfamonometoxina e sulfisoxazol. Os compostos assim obtidos foram submetidos as analises classicas, espectrofotometricas e de ressonancia magnetica protonica

Certain aspects of dapsone metabolism in leprosy patients as studied by high performance liquid chromatography (HPLC) and qualitative screening tests.

Dapsone (DDS) in urine of 250 leprosy patients collected on surprise visits were screened by simple paper spot, tile tests and sensitive Enzyme linked immunosorbent assay (ELISA) and Haemagglutination inhibition (HI) tests. The urinary DDS concentration as well as DDS/C ratios were also studied. Simultaneously, 50 microliter of blood was collected from each of these patients and its dapsone content was estimated by HPLC. Urine samples with means of 25 to 30 micrograms/ml DDS and 55-64 micrograms/mg DDS/C ratios were found to give positive tests by any of the above screening procedures, while their mean blood DDS concentration was found to be 0.91 microgram/ml. The corresponding values for those specimens giving negative tests were 3.8 to 5.7 micrograms DDS per ml and 9 to 13 micrograms/mg DDS/C ratio. The blood DDS concentration in this group was ranging from 0.16 to 0.18 micrograms/ml. The findings are discussed in relation to their metabolic significance and their application in a leprosy control programme.