gem-Dithioacetylated indole derivatives as novel antileishmanial agents |
| |
Authors: | Sharad Porwal Suman Gupta Prem M.S. Chauhan |
| |
Affiliation: | 1. Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India;2. Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India |
| |
Abstract: | In this communication we report a serendipitously discovered hybrid molecule 1, combining fragment of 3 (an in vivo active antileishmanial molecule) with H2S donor moiety (known for bimodal behavior of cytoprotection and apoptosis), as antileishmanial agent. Compound 1 suppresses 99.82% parasitemia of L. donovani infected macrophages at 12.5 μg/ml without even deforming them (CC50 > 100 μg/ml). This compound appears cytotoxic for intracellular amastigotes while cytoprotective to host macrophages. The concept can be utilized to develop high therapeutic index NCE (New Chemical Entities) for other macrophage mediated diseases like tuberculosis and cancer. |
| |
Keywords: | Hybrid Antileishmanial Cyctoprotection |
本文献已被 ScienceDirect 等数据库收录! |
|