Combinatorial Chemistry & High Throughput Screening

Rathnam Chaguturu 
iDDPartners, 3 Edith Court
Princeton Junction
NJ 08550


Synthesis of Combinatorial Libraries Based On Terpenoid Scaffolds

Author(s): A. Pathak, S. K. Singh, M.A. Farooq Biabani, D. K. Kulshreshtha, S. K. Puri, S. Srivastava and B. Kundu

Affiliation: Medicinal ChemistryDivision, Central Drug Research Institute, Lucknow 226 001, India


Triterpenoid-based scaffolds betulinic acid (1a) and ursolic acid (1b), have been used for the generation of combinatorial libraries in parallel format using solid phase organic synthesis method. These templates have the potential for the synthesis and amplification of triterpenoid-based compounds with one and two-point diversity. This has been demonstrated by the synthesis of two small libraries comprising 18 derivatives each of betulinic acid and ursolic acid with structural diversity at C-3 and C-28 positions. The primary screening of antimalarial activity of these libraries against P. falciparum in vitro led to the identification of four compounds with 5 fold increase in the activity compared to betulinic and ursolic acids.

Keywords: terpenoid scaffolds, betulinic acid, ursolic acid

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Article Details

Page: [241 - 248]
Pages: 8
DOI: 10.2174/1386207024607275
Price: $58