In vivo and in vitro antimalarial effect and toxicological evaluation of the chloroquine analogue PQUI08001/06.

Antimalarial interventions mostly rely upon drugs, as chloroquine. However, plasmodial strains resistant to many drugs are constantly reported, leading to an expansion of malaria cases. Novel approaches are required to circumvent the drug resistance issue. Here, we describe the antimalarial potential of the chloroquine analogue 2-[[2-[(7-chloro-4-quinolinyl)amino]ethyl]amino] ethanol (PQUI08001/06). We observed that PQUI08001/06 treatment reduces parasitemia of both chloroquine-resistant and -sensitive strains of Plasmodium falciparum in vitro and P. berghei in vivo. Our data suggests that PQUI08001/06 is a potential antimalarial therapeutic alternative approach that could also target chloroquine-resistant plasmodial strains.

7-Chloro-4-[(E)-2-(4-methoxy-benzyl-idene)hydrazin-1-yl]quinoline monohydrate.

The organic mol-ecule in the title hydrate, C(17)H(14)ClN(3)O·H(2)O, has a small but significant twist from planarity, as seen in the dihedral angle of 12.10 (17)° between the quinoline and benzene rings. The conformation about the C=N bond is E. Chains along the b axis are formed in the crystal structure aided by water-quinoline O-H⋯N (× 2) and hydrazone-water N-H⋯O hydrogen bonds. Layers of these chains stack along the a axis via C-H⋯π and π-π inter-actions [ring centroid-ring centroid distance = 3.674 (2) Å]. C-H⋯O inter-actions are also present.

N-(4-Bromo-phen-yl)pyrazine-2-carbox-amide.

The mol-ecule of the title compound, C(11)H(8)BrN(3)O, is close to planar (r.m.s. deviation of all 16 non-H atoms = 0.103 Å), a conformation stabilized by an intra-molecular N-H⋯N hydrogen bond, which generates an S(5) ring. In the crystal structure, supra-molecular chains mediated by C-H⋯O contacts (along a) are linked into a double layer via N⋯Br halogen bonds [3.207 (5) Å] and C-Br⋯π inter-actions [Br⋯ring centroid(pyrazine) = 3.446 (3) Å]. The layers stack along the b axis via weak π-π inter-actions [ring centroid(pyrazine)⋯ring centroid(benzene) distance = 3.803 (4) Å].

Synthesis and biological evaluation of N-(aryl)-2-thiophen-2-ylacetamides series as a new class of antitubercular agents.

The present article describes a series of 21 N-(aryl)-2-thiophen-2-ylacetamides, which were synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis, and the activity expressed as the minimum inhibitory concentration (MIC) in mug/mL. The compounds 2, 3, 7, 8, 11, 12, 15, 16, and 20 exhibited activity between 25 and 100 microg/mL and could be a good start point to find new lead compounds in the fight against multidrug resistant tuberculosis.