9-Anilinoacridines as 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-...

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...

Glucan and Tuftsin - Potential Antileishmanial Agents

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...

N-cinnamoylated aminoquinolines as promising antileishmanial agents.

A series of cinnamic acid conjugates of primaquine and chloroquine were evaluated for their in vitro antileishmanial activities. Although primaquine derivatives had modest activity, chloroquine conjugates exhibited potent activity against both promastigotes (50% inhibitory concentration [IC50] = 2.6 to 21.8 μM) and intramacrophagic amastigotes (IC50 = 1.2 to 9.3 μM) of Leishmania infantum. Both...