5-Nitroisatin-derived thiosemicarbazones: potential antileishmanial agents

9-Anilinoacridines as potential antileishmanial agents.

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-...

Glucan and Tuftsin - Potential Antileishmanial Agents

1,3‐Bis(aryloxy)propan‐2‐ols as potential antileishmanial agents

We describe herein the synthesis and antileishmanial activity of 1,3-bis(aryloxy)propan-2-ols. Five compounds (2, 3, 13, 17, and 18) exhibited an effective antileishmanial activity against stationary promastigote forms of Leishmania amazonensis (IC50  < 15.0 μm), and an influence of compound lipophilicity on activity was suggested. Most of the compounds were poorly selective, as they showed tox...

Nitroimidazooxazoles# Part xxiv, Search for Antileishmanial Agents: 2,3-Dihydro-6-nitroimidazo[2,1-b]oxazoles as Potential Antileishmanial Agents

A number of mono and bicyclic nitroimidazoles were screened for in vitro antileishmanial activity. Among these, compounds belonging to the class of nitroimidazo[2,1-b]oxazoles showed moderate to good activity. This class of compounds had been reported previously to have pronounced antitubercular activity, particularly CGI17341 (5a). In the present study (5a) and (5d) and (7) were found to be mo...

Liposomal Delivery of Antileishmanial Agents

Initially, the use of liposomes was mainly confined to model membrane systems, however, recently their use as vehicles for transfer of genetic and other materials into cells in cultures or for drug delivery to desired cellular and subcellular sites in a living system has been the subject of discussion. Liposomes can vary widely in size, chemical composition, and surface characteristics; they ca...