Margarita Suárez Navarro

Effect of thiadiazine derivatives on intracellular amastigotes of Leishmania amazonensis.

Current therapy for leishmaniasis is not satisfactory. We describe the in vitro antiproliferative effects of new thiadiazine derivatives against Leishmania amazonensis. The compounds were found to be active against the amastigote form of the parasite, inhibiting parasite growing, from 10 to 89%, at a concentration of 100 ng/ml. This activity suggests that thiadiazine derivatives could be considered as potential antileishmanial compounds.

Thiadiazine Derivatives as Antiprotozoal New Drugs

The 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione scaffold have found many applications in recent years. This review is aimed at highlighting the most important aspects about these compounds: synthesis, spectroscopic characterization and antiprotozoan activities. How the chemical nature of N-substituents influences the overall activity / cytotoxicity profile will also be discussed.

Ethyl methyl 1,4-dihydro-4-(3-nitrophenyl)-2, 6-bis(1-piperidylmethyl)pyridine-3,5-dicarboxylate.

In the title compound, C(28)H(38)N(4)O(6), the 4-aryl substituent occupies a pseudo-axial position approximately orthogonal to the plane of the dihydropyridine ring [88.1 (3) degrees ]. The dihydropyridine ring adopts a flattened boat conformation. The H atom on the pyridine N atom is involved in a bifurcated intramolecular hydrogen bond, the acceptors being the N atoms of the two piperidylmethyl groups [N.N 2.629 (4) and 2.695 (4) A].

3,3,6,6-Tetramethyl-9-(3-nitrophenyl)-3,4,5,6,9,10-hexahydroacridine-1,8(2H,7H)-dione

In the title compound, C 23 H 26 N 2 O 4 , the central ring adopts a distorted boat conformation, while the two outer rings are almost in ideal envelope conformations. The molecular packing is stabilized by van der Waals interactions and hydrogen bonds.

3‐(2‐Hydroxyphenylamino)‐5,5‐dimethylcyclohex‐2‐enone

In the title compound, C 14 H 17 NO 2 , the molecules are linked through two hydrogen bonds to form a two-dimensional network in the (100) plane. The carbonyl-O atom is involved in two intermolecular hydrogen bonds, one with the amino group and the other with the hydroxy group. The cyclohexenone ring is disordered into two distorted half-chair conformations. The phenyl and cyclohexenone moieties are not coplanar.

5-Methoxycarbonyl-6-methyl-4-phenyl-3,4-dihydro-2(1H)-pyridone

Crystals of the title compound, C 14 H 15 NO 3 are stabilized by intermolecular hydrogen bonds between the NH group and one O atom of the carbonyl group. The six-membered ring adopts a twist conformation and the lactone ring a planar conformation.