A Living Topochemical Ring-Opening Polymerization of Achiral Amino Acid N-Carboxy-Anhydrides in Single Crystals.

A living topochemical ring-opening polymerization (ROP) of achiral amino-acid N-carboxyanhydrides (NCAs) is reported. Single crystals of the NCAs of α-aminoisobutyric acid (Aib) and 1-aminocyclohexanecarboxylic acid (ACHC) were grown, allowing a ring-opening polymerization macroscopically induced by amines. The single crystals could be polymerized at temperatures from 25-50 °C after physically contacting the amine-based initiator with the crystals.

Secondary Structures in Synthetic Poly(Amino Acids): Homo- and Copolymers of Poly(Aib), Poly(Glu), and Poly(Asp).

The secondary structure of poly(amino acids) is an excellent tool for controlling and understanding the functionality and properties of proteins. In this perspective article the secondary structures of the homopolymers of oligo- and poly-glutamic acid (Glu), aspartic acid (Asp), and α-aminoisobutyric acid (Aib) are discussed. Information on external and internal factors, such as the nature of side groups, interactions with solvents and interactions between chains is reviewed.

Novel 12-hydroxydehydroabietylamine derivatives act as potent and selective butyrylcholinesterase inhibitors.

The skeleton of the diterpene dehydroabietylamine was modified, and a set of 12-hydroxy-dehydroabietylamine derivatives was obtained. The compounds were screened in colorimetric Ellman's assays to determine their ability to act as inhibitors for the enzymes acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine serum). Additional investigations concerning the enzyme kinetics were performed and showed 12-hydroxy-N-(4-nitro-benzoyl)dehydroabietylamine (13) and 12-hydroxy-N-(isonicotinoyl)dehydroabietylamine (17) as selective BChE inhibitors holding good inhibition constants K = 0.

Syntheses of C-ring modified dehydroabietylamides and their cytotoxic activity.

Due to their auspicious pharmacological efficacy as future drug candidates, natural products have been attracting scientific interest for centuries. An interesting field of research concerns the natural product class of terpenes. In this regard, a multitude of studies have already shown their promising biological potential.