4-Chlorophenylthioacetone-derived thiosemicarbazones as potent antitrypanosomal drug candidates: Investigations on the mode of action.

Chagas disease (ChD), caused by Trypanosoma cruzi, remains a challenge for the medical and scientific fields due to the inefficiency of the therapeutic approaches available for its treatment. Thiosemicarbazones and hydrazones present a wide spectrum of bioactivities and are considered a platform for the design of new anti-T. cruzi drug candidates.

A Comprehensive View on (-)-7-Oxo-ent-kaur-16-en-19-oic Acid, the Major Constituent of Xylopia sericea Leaves Extract: Complete NMR Assignments, X-Ray Crystallographic Structure, in Vitro Antimalarial Activity and Cytotoxicity.

Bioguided fractionation of Xylopia sericea antiplasmodial dichloromethane leaves extract led to the isolation of (-)-7-oxo-ent-kaur-16-en-19-oic acid (C H O ) that was identified by a combination of 1D and 2D NMR experiments (COSY, HMBC, HSQC, HSQC-TOCSY, HSQC-NOESY and NOESY) and by X-ray crystallography. A feature to be pointed out is its (4R) configuration that was inferred from the NOE experiments (HSQC-NOESY and NOESY) and X-ray crystallography. In vitro evaluation of this rare diterpene acid against the chloroquine-resistant strain Plasmodium falciparum W2 by the PfLDH method showed it disclosed a low antiplasmodial activity and was not cytotoxic to HepG2 cells (CC 862.

Two polymorphs of 2-(prop-2-yn-1-yl-oxy)naphthalene-1,4-dione: solvent-dependent crystallization.

The title compound, CHO, crystallizes in two polymorphs, namely the monoclinic (space group 2/) and triclinic (space group ī) forms, obtained from ,-di-methyl-formamide and isopropyl alcohol solutions, respectively. The mol-ecular structures and conformations in the two forms are essentially the same as each other. The naphtho-quinone ring systems are essentially planar with r.

Crystal structure of 2-hy-droxy-3-(prop-2-yn-1-yl)naphthalene-1,4-dione.

The naphtho-quinone unit of the title compound, CHO, is essentially planar, with an r.m.s.

Crystal structure of 4-nitro-phenyl 6--ethyl-β-d-galacto-pyran-oside monohydrate.

The synthesis and crystal structure of the title compound, CHNO·HO, prepared in three steps from 6--ethyl-1,2;3,4-di--iso-propyl-idene-α-d-galacto-pyran-ose using protecting-group strategies employed in carbohydrate chemistry, is reported. The asymmetric unit consists of a single galactoside mol-ecule, in which the pyran-oid ring has a conformation and the 4-nitro-phenyl moiety is essentially planar. In the crystal, each carbohydrate is surrounded by other d-galactose residues and water mol-ecules, linked by O-H⋯O hydrogen bonds involving all hy-droxy groups, giving a two-dimensional substructure lying parallel to (100) and extended into three dimensions by C-H⋯O inter-actions.

Nanoparticle phosphate-based composites as vehicles for antimony delivery to macrophages: possible use in leishmaniasis.

Pentavalent antimonial drugs such as N-methylglucamine antimonate (Glucantime®) are used for treating leishmaniasis but produce severe side effects, including cardiotoxicity and hepatotoxicity. We characterized the physicochemical properties of 3 nanoparticle phosphate-based composites (NPCs; NPC0, NPC3, and NPC5) as Sb(v) carriers for specifically targeting macrophages and reducing systemic side effects. NPCs were synthesized in liquid media and sterilized at 25 kGy before use.