2. Academic Validation
  3. Chemotherapy of leishmaniasis. Part XII: design, synthesis and bioevaluation of novel triazole integrated phenyl heteroterpenoids as antileishmanial agents

Chemotherapy of leishmaniasis. Part XII: design, synthesis and bioevaluation of novel triazole integrated phenyl heteroterpenoids as antileishmanial agents

  • Bioorg Med Chem Lett. 2013 May 15;23(10):2925-8. doi: 10.1016/j.bmcl.2013.03.055.
S N Suryawanshi 1,  Avinash Tiwari,  Santosh Kumar,  Rahul Shivahare,  Monika Mittal,  Padam Kant,  Suman Gupta
Affiliations

Affiliation

  • 1 Division of Medicinal Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 001, India.
PMID: 23582274 DOI: 10.1016/j.bmcl.2013.03.055
Abstract

A novel series of triazole integrated phenyl heteroterpenoids have been synthesized and screened for their in vitro activity against intracellular amastigote form of Leishmania donovani. Among all tested compounds, compound 3a was found to be the most active with IC50 6.4μM and better selectivity index (SI) 18 as compared to reference drugs, miltefosine and miconazole. When evaluated in vivo in L. donovani/hamster model, 3a has exhibited 79±11% inhibition of Parasite multiplication at 50mgkg(-1)×5days on day 7 post treatment.

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