Leishmaniasis, caused by the protozoan parasites of the genus Leishmania, is one of the most neglected diseases endemic in many continents posing enormous global health threats and therefore the discovery of new antileishmanial compounds is of utmost urgency. The antileishmanial activities of a library of sugar amino acid-based linear lipopeptide analogues were examined with the aim to identify...

This work describes an analytical platform based on semi-high-resolution antileishmanial profiling combined with hyphenation of high-performance liquid chromatography - high-resolution mass spectrometry - solid-phase extraction - nuclear magnetic resonance spectroscopy, i.e., semiHR-antileishmanial assay/HPLC-HRMS-SPE-NMR. The platform enables fast pinpointing of HPLC peaks representing Leishma...

A number of 1'-substituted 9-anilinoacridines were evaluated for their activities against promastigote and amastigote forms of Leishmania major and for their toxicities to human Jurkat leukemia cells. Several compounds possessing 1'-NH-alkyl substituents produced more than 80% growth inhibition of macrophage-infected L. major amastigotes at or below a concentration of 1 microM. 1'-Hexylamino-9-...

Quantitative structure-activity relationship (QSAR) studies were performed in order to identify molecular features responsible for the antileishmanial activity of 61 adenosine analogues acting as inhibitors of the enzyme glyceraldehyde 3-phosphate dehydrogenase of Leishmania mexicana (LmGAPDH). Density functional theory (DFT) was employed to calculate quantum-chemical descriptors, while several...

leishmaniasis is a neglected public health problem caused by the protozoan species belonging to the genus leishmania affecting mostly the poor populations of developing countries. the causative organism is transmitted by female sandflies. cutaneous, mucocutaneous, and visceral clinical manifestations are the most frequent forms of leishmaniasis. chemotherapy still relies on the use of pentavale...

leishmaniasis has a wide spectrum of signs and symptoms due to infection to numbers of leishmania species and makes enormous mortality and morbidity. there are clues of antileishmanial effects of prenylated coumarins. apiaceae family is one of the most important sources of coumarins. air-dried aerial parts of ferulago angulata and fruits of prangos asperula were extracted with n -hexane, using ...

The World Health Organization has classified the leishmaniasis as a major tropical disease. An effective vaccine against leishmaniasis is not available and chemotherapy is the only effective way to treat all forms of disease. However, current therapy is toxic, expensive and the resistance has emerged as a serious problem, which has compelled the search for new antileishmanial agents. The aim of...

Crude ethanolic extract, lignoid fraction and the purified compound yangambin were obtained from Ocotea duckei (Lauraceae) and their antileishmanial activity was tested against promastigote forms of Leishmania chagasi and Leishmania amazonensis cultivated in Schneider medium, supplemented with 20% of fetal bovine serum. All substances presented antileishmanial activity with IC50 values of 135.7...

Leishmaniasis is a complex vector-borne protozoan disease caused by parasites of the genus Leishmania. The parasites hugely vary in their mode of tropism giving rise to different non-lethal to fatal clinical patterns of the disease. Afflicting millions, the disease is endemic in tropics and sub-tropics, where majority of the affected individuals are rural and unsound economically, leading to it...

In continuation of our natural and medicinal research programme on tropical rainforest plants, a bioassay guided fractionation of ethanolic extract of leaves of Canarium patentinervium Miq. (Burseraceae Kunth.) led to the isolation of scopoletin (1), scoparone (2), (+)-catechin (3), vomifoliol (4), lioxin (5), and syringic acid (6). All the compounds exhibited antiacetylcholinesterase activity ...