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1.
Chem Biodivers ; 20(7): e202300191, 2023 Jul.
Article in English | MEDLINE | ID: mdl-37294393

ABSTRACT

The regiospecific reduction of 4,6-dinitrobenzimidazole derivatives leading to the corresponding 4-amino-6-nitrobenzimidazoles was studied. The identification of the formed product structures was accomplished by spectroscopic and X-ray diffraction data. The anticancer and antiparasitic activities of the synthesized compounds were examined, and promising activities against Toxoplasma gondii and Leishmania major parasites were discovered for certain 4,6-dinitrobenzimidazoles in addition to moderate anticancer activities of the 4-amino-6-nitrobenzimidazole derivatives against T. gondii cells. However, the tumor cell experiments revealed a promising sensitivity of p53-negative colon cancer cells to these compounds.


Subject(s)
Leishmania major , Toxoplasma , Antiparasitic Agents/pharmacology , Antiparasitic Agents/chemistry
2.
Acta Crystallogr E Crystallogr Commun ; 71(Pt 9): o684-5, 2015 Sep 01.
Article in English | MEDLINE | ID: mdl-26396904

ABSTRACT

The reaction of 5-methyl-7-nitro-1H-indole-2-carbohydrazide with ethyl aceto-acetate yielded the title mol-ecule, C16H18N4O5, in which the indole ring is almost planar, with the greatest deviation from the mean plane being 0.006 (2) Å. The nine atoms of the indole ring are almost perpendicular to the mean plane through the ethyl acetate group, as indicated by the dihedral angle of 87.02 (4)° between them. In the crystal, centrosymmetric supra-molecular dimers are formed via N-H⋯O hydrogen bonds and eight-membered amide {⋯HNCO}2 synthons. These are consolidated into a three-dimensional architecture by C-H⋯O contacts, and by π-π inter-actions between six-membered rings [inter-centroid distance = 3.499 (2) Å].

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