CHEMICALLY ENGINEERED EXTRACTS AS ALTERNATIVE SOURCE OF BIOACTIVE COMPOUNDS

MENDEZ, L; SALAZAR, MO; RAMALLO, IA; FURLAN, RLE

Santiago de Compostela

Simposio; II Simposio Iberoamericano de Química Orgánica; 2010

Diferentes sociedades de química iberoamericanas

The access to libraries of molecules with interesting biomolecular properties is a limiting step in the drug discovery process. By virtue of a long molecular evolution process, natural products are recognized as biologically validated starting points in structural space for library development. We discuss here a strategy to generate natural product-like libraries. Semi synthetic mixtures of compounds are produced by diversification of natural product extracts through chemical transformation of common chemical functionalities in natural products into chemical functionalities rarely found in nature. Natural extracts are transformed by reaction with hydrazine, arylsulfonyl chlorides and bromine. The effect of such reactions on the chemical composition and on different biomolecular properties will be discussed as well as some examples of compounds isolated by bioguided fractionation of chemically engineered extracts.