Synthesis of new uracil-5-sulphonamide-p-phenyl derivatives and their effect on Biomphalaria alexandrina snail's nucleoproteins.
In continuation of the previous work (Fathalla, 1992) on the synthesis of some heterocycles containing uracil moiety, we report herein the incorporation of uracil moiety into cyanopyridine thione, thiosemecarbazone, semicarbazone, cyanopyridine, aminocyano pyridine, isoxazoline, pyrazoline, pyrimidine, triazolo pyrimidine, pyran, selena and thiazole derivatives which might modify their biological activities. The biological studies revealed that the chemical compound III f showed high molluscicdal activity than other compounds. The profile of the nucleoprotein extracted from chemically (compound IIIc, e, f and g) treated or UV-irradiated B. alexandrina snails did not show appreciable differences when compared to non-treated (native) snails by using SDS-PAGE, where no obvious qualitative or quantitative differences were observed. Immunization of experimental animals with the nucleoprotein extracted from native, chemically (compound III f & g) treated or physically treated B. alexandrina snails induced significant protection against challenge with normal S. mansoni cercariae, as compared to the non-immunized challenged control. As well as, a decrease in the number of granuloma formation and the size range of granuloma was also observed in immunized animals. It is concluded that, compounds III f and g have a potent molluscicidal activity. They also induced chemical modification comparable to that induced by physical treatment in the snail's nucleoprotein, which could possibly be used in immunization against S. mansoni infection.
Fathalla
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Medicinal Chemistry Department, National Research Center, Cairo, Egypt. omarfathalla@yahoo.com
Gad
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Maghaby
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D000818:Animals; D001700:Biomphalaria / Q000378:metabolism* / Q000469:parasitology*; D004591:Electrophoresis, Polyacrylamide Gel; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D008975:Molluscacides / Q000138:chemical synthesis* / Q000633:toxicity; D009698:Nucleoproteins / Q000737:chemistry / Q000187:drug effects*; D012550:Schistosoma mansoni / Q000187:drug effects; D012744:Sex Ratio; D013055:Spectrophotometry, Infrared; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000633:toxicity; D014498:Uracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000633:toxicity
D008975:Molluscacides; D009698:Nucleoproteins; D013449:Sulfonamides; D014498:Uracil