Activity of 1-aryl-4-(naphthalimidoalkyl) piperazine derivatives against Leishmania major and Leishmania mexicana.

A series of 1-aryl-4-(phthalimidoalkyl) piperazines and 1-aryl-4-(naphthalimidoalkyl) piperazines were retrieved from a proprietary library based on their high structural similarity to haloperidol, an antipsychotic with antiparasitic activity, and assessed as potential antileishmanial scaffolds. Selected compounds were tested for antileishmanial activity against promastigotes of Leishmania major and Leishmania mexicana in dose-response assays. Two of the 1-aryl-4-(naphthalimidoalkyl) piperazines (compounds 10 and 11) were active against promastigotes of both Leishmania species without being toxic to human fibroblasts. Their activity was found to correlate with the length of their alkyl chains. Further analyses showed that compound 11 was also active against intracellular amastigotes of both Leishmania species. In promastigotes of both Leishmania species, compound 11 induced collapse of the mitochondrial electrochemical potential and increased the intracellular Ca2+ concentration. Therefore, it may serve as a promising lead compound for the development of novel antiparasitic drugs.

Differences in Nutritional and Health Status in School Children from the Highlands and Lowlands of Bolivia.

Children in the Bolivian Andes are exposed to endemic infections and meager nourishment, and live under poor hygienic conditions. The prevention of children malnutrition is a priority in many countries including Bolivia. In this study, the health status of schoolchildren in Taraco, a Puna district, at 4,000 meters above sea level (masl) and in Caranavi, at 650 masl in the wealthier subtropical valleys, was compared. The weight, height, and hematological and biochemical parameters in blood, parasites in stool, and clinical information in 120 children from rural Taraco and in 96 from semi-urban Caranavi, both predominantly of Aymara ethnicity, were registered. Eleven percent of Taraco children were undernourished compared with 3% in Caranavi. Instead, 41% of the children in Caranavi were obese or overweight, compared with 8% in Taraco. Anemia was found in 74% of the children in Taraco compared with 7% in Caranavi. Albumin levels were normal in all samples, albeit lower in Taraco. Similar and normal serum zinc levels were measured in both groups. Approximately 60% of the children in both locations showed insufficient vitamin D levels, with lower levels in Taraco children. Hymenolepis nana and Entamoeba coli, parasites determinant of poor hygienic conditions, were respectively detected in 78% and 21% of fecal samples from Taraco, and in 29% and 8% of samples from Caranavi. We show increased anemia, nutritional deficiencies, and indications of poor hygienic conditions in highlands compared with lowlands. The prevalence of obesity in the lowlands demands addressing diverse nutritional deficiencies in the regions of Bolivia.