期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 20, 页码 4643-4646出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.09.018
关键词
Hybrid; H2S donor; Antileishmanial; Cyctoprotection
资金
- CSIR, New Delhi
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 mu g/ml without even deforming them (CC50 > 100 mu g/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. (c) 2017 Elsevier Ltd. All rights reserved.
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