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  • Title: Synthesis of new quinazolin-2,4-diones as anti-Leishmania mexicana agents.
    Author: Enciso E, Sarmiento-Sánchez JI, López-Moreno HS, Ochoa-Terán A, Osuna-Martínez U, Beltrán-López E.
    Journal: Mol Divers; 2016 Nov; 20(4):821-828. PubMed ID: 27531196.
    Abstract:
    The quinazolin-2,4-dione moiety is found in many compounds with important biological activities making it a target for its synthesis. In this work, a one-pot three-step synthesis of new quinazolin-2,4-diones from phthalic anhydrides and their activity against Leishmania mexicana are described. The new quinazolin-2,4-diones were isolated with yields in the range of 32-70 %. All compounds displayed lower cytotoxicity in RAW 264.7 macrophage over miltefosine. Compound 6,7-dichloro-3-phenylquinazoline-2,4(1H,3H)-dione (6e) displayed an attractive profile which includes anti-Leishmania mexicana activity ([Formula: see text] [Formula: see text]M), much lower cytotoxic activity ([Formula: see text] [Formula: see text]M) and a high selective index ([Formula: see text]) proving to be superior to miltefosine.
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