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NEW DERIVATIVES OF BISNAFTALIMIDOPROPIL, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND ITS USE IN CANCERIAN AND PARASITIC DISEASES, ESPECIALLY LEISHMANIOSIS, TRYPANOSOMES AND MALARIA.
NEW DERIVATIVES OF BISNAFTALIMIDOPROPIL, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND ITS USE IN CANCERIAN AND PARASITIC DISEASES, ESPECIALLY LEISHMANIOSIS, TRYPANOSOMES AND MALARIA.
The present invention relates to the collection of new derivatives of bisnisolipidopropyl and its use in the treatment of cancers and parasitic diseases. THE FOLLOWING DERIVATIVES OF BISNAFTALIMIDOPROPIL OF GENERAL FORMULA A (FIG. 1), IN WHICH (A) THE DIVERSITY POINT REPRESENTS: BNIPPUT, BNIPDAPEN, BNIPDAHEX, BNIPDAHEP, BNIPDAOCT, BNIPDANON, BNIPDADAN, BNIPDADOD, BNIPDPTA and BNIPDETA). It was found that the yield of synthesis was around 50 to 70%. Its cytotoxicity, against tumor cells (CACO-2) and against Leishmania infantum parasite were evaluated by the MTT method and by the activity of LUCIFERASE present in PARASITE, RESPECTIVELY. CITROXICITY IN COCO-2 CELLS WAS MANIFESTED WITH IC50 VALUES BETWEEN 0.3 AND 22 ONE, AFTER 48 HOURS OF INCUBATION WITH THE COMPOUNDS. THE VALUES OF IC50 AGAINST LEISHMANIA INFANTUM VARY FROM 0.39 TO 2.09 UM FOR THE PROMASTIGOTE FORM, BETWEEN 5.24 AND 17.42 ONE, TO THE AMXTINIC AMASTIGOTA FORM AND BETWEEN 2.43 TO 9.52 UM, FOR THE INTRACELLULAR AMASTIGOTA FORM. THESE COMPOUNDS REPRESENT AN ALTERNATIVE TO THE THERAPEUTICS EXISTING FOR THE REFERENCED AREAS, AND CAN SOLVE THE PROBLEMS OF TOXICITY AND RESISTANCE IN RELATION TO THE COMPOUNDS EXISTING IN THE MARKET.
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