Collect. Czech. Chem. Commun. 1996, 61, 171-231

Molecular Diversity and Libraries of Structures: Synthesis and Screening

Markéta Rinnováa and Michal Leblb

a Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 166 10 Prague 6, Czech Republic
b Selectide Corporation, An Affiliate of Hoechst Marion Roussel, 1580 E. Hanley Blvd., Tucson, AZ 85737, U.S.A.


Library, or molecular diversity, approaches are a progressive tool in contemporary investigation of biological interactions and drug discovery. All library approaches include certain degree of rationality and cannot be therefore classified as random or irrational techniques. Reviewed techniques are complementary to so called "rational design"; they can serve either as a tool to generate a lead, or, on the other hand, to optimize a "designed" lead by rapid evaluation of structure-activity relationships. Combinatorial approaches are based on either a random or multiple principle which enables production of large number of diverse molecular structures that can be simultaneously screened and evaluated in a biological assay to find an optimal interacting molecule.

Keywords: Combinatorial libraries; Multiple syntheses; Solid phase syntheses; Biological libraries.