2. Academic Validation
  3. Chemotherapy of leishmaniasis part XIII: design and synthesis of novel heteroretinoid-bisbenzylidine ketone hybrids as antileishmanial agents

Chemotherapy of leishmaniasis part XIII: design and synthesis of novel heteroretinoid-bisbenzylidine ketone hybrids as antileishmanial agents

  • Bioorg Med Chem Lett. 2015 Jan 15;25(2):410-3. doi: 10.1016/j.bmcl.2014.09.078.
Avinash Tiwari 1,  Santosh Kumar 1,  Rahul Shivahare 2,  Padam Kant 3,  Suman Gupta 2,  S N Suryawanshi 4
Affiliations

Affiliations

  • 1 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
  • 2 Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
  • 3 Department of Chemistry, University of Lucknow, Lucknow 226 001, India.
  • 4 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India. Electronic address: shivajins@yahoo.co.in.
PMID: 25475205 DOI: 10.1016/j.bmcl.2014.09.078
Abstract

Some novel heteroretinoid-bisbenzylidine ketone hybrids have been synthesized and evaluated for their in vitro antileishmanial activity against intramacrophagic amastigotes of Leishmania donovani. Among all the nine synthetic compounds, five compounds (7c, 7d and 7f-h) have shown significant (less than 7μM) activity against intramacrophagic amastigotes. The IC50 values of these compounds were found better than the reference drugs sodium stibogluconate (SSG) and miltefosine. This study helped us in identifying the new class of compounds that could be exploited as potent antileishmanial agents.

Keywords

Bisbenzylidine ketone; Heteroretinoid; In vitro activity; Leishmania donovani.

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