The Pictet-Spengler condensation: a new direction for an old reaction

Article Abstract:

Trans isomers of beta-carbolines are formed by the Pictet-Spengler condensation reaction of N(sub b)-benzyl-tryptophan alkyl esters with aldehydes. The beta-carbolines formed are highly distereoselective and function as inverse agonist ligands of the GABA receptors in the central nervous system. The study of ligand agonists and inverse agonists is necessary to develop psychoactive drugs. The synthesis of (-)-alstonerine and (+)macroline using a ketone formed by the Pictet-Spengler condensation is given.

Condensation products (Chemistry)

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Chemistry and structural biology of androgen receptor

Article Abstract:

A review on well-characterized androgen receptor (AR) ligands that bind to the AR with high affinity and discussion regarding the biology, metabolism, and structure-activity relationships for therapeutic and emerging classes of AR ligands is presented. Novel nonsteroidal pharmacophores is summarized with discussion of the emerging structure-activity relationships and examples of their tissue selectivity included.

Science & research, Androgens, Chemical properties

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Transition-metal complexes containing trans-spanning diphosphine ligands

Article Abstract:

Two approaches for the synthesis of transition-metal complexes containing bidentate trans-spanning tertiary phophine ligands, the preformed ligand startegy and the in situ ligand strategy, are described. Research reveals that the preformed ligand strategy is more successful than the other and the synthesized compounds exhibit unusual metal geometries.

Statistical Data Included, Analysis, Chemical structure, Transition metal compounds

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