Antileishmanial activity of benzocycloalkyl azole oximino ethers: The conformationally constraint analogues of oxiconazole

作者：Verma Aditya; Srivastava Saumya; Sane Shraddha A; Marrapu Vijay K; Srinivas Nagarapu; Yadav Manisha; Bhandari Kalpana; Gupta Suman^*

来源：Acta Tropica, 2011, 117(2): 157-160.

DOI：10.1016/j.actatropica.2010.10.011

• Visceral leishmaniasis
• Antileishmanial activity
• Benzocycloalkyl azole oximino ethers
• Luciferase assay

Antileishmanial activities of 16 synthetic oximino benzocycloalkyl azoles against Leishmania donovani were evaluated in vitro against extracellular promastigotes and intracellular amastigotes. Based on SI (Selectivity Index), five compounds were tested further in vivo in hamster model. Out of these, three compounds have shown medium activity (53-58%) and one has shown significant inhibition of parasite multiplication (70%). Despite the fact that these compounds were better than the existing antileishmanials in respect to IC(50) and SI values, they were less active than miltefosine in vivo. The present study has helped us in identifying a new lead that could be exploited as a potential antileishmanial agent.

• 出版日期2011-2