Synthesis and characterization of random and block copolypeptides derived from gamma-methylglutamate and leucine N-carboxyanhydrides.

The synthesis of random and block copolypolyeptides derived from gamma-methylglutamate and leucine N-carboxyanhydrides using Al-Schiff's base complexes and allylamine as initiators is here reported. The copolymer structures were confirmed by (1)H and (13)C NMR. The calculation of the statistical average block lengths reveals the presence of longer methylglutamate units in the copolymer.

Biomimetic poly(methyl methacrylate)-based terpolymers: modulation of bacterial adhesion effect.

Adherence of Staphylococcus aureus, responsible for major foreign body infections, was assessed onto functionalized poly(methyl methacrylate)-based terpolymers bearing sulfonate and carboxylate groups and onto poly(methyl methacrylate) as control. These terpolymers, have been synthesized by radical copolymerization of methyl methacrylate, methacrylic acid, and sodium styrene sulfonate by varying the ratio R = [COO(-)]/[COO(-) + SO(3)(-)] from 0 to 1 and keeping ionic monomer content between 7 and 18%. Adsorption of fibronectin onto poly(methyl methacrylate) was shown to dramatically promote bacterial adherence, whereas a strong inhibition of bacteria adherence was observed onto functionalized terpolymers containing both carboxylate and sulfonate groups.

Progesterone freeze-dried systems in sublingual dosage form.

Various polymer matrices were tested to enhance progesterone bioavailability as part of an emergency therapy. Among the different polymers used, i.e.

Delta opioid receptor selectivity induced by conformational constraints in linear enkephalin-related peptides: 1H 400-MHz NMR study and theoretical calculations.

Introduction into the structure of the linear hexapeptide DSLET (Tyr-D-Ser-Gly-Phe-Leu-Thr) or DTLET (Tyr-D-Thr-Gly-Phe-Leu-Thr) of tert-butyl groups as constraints different from cyclization leads to a large increase in the selectivity for delta opioid binding site in the case of DSTBULET [Tyr-D-Ser-(OtBu)-Gly-Phe-Leu-Thr] (Ki delta = 6.14 nM; Ki mu = 374 nM) and BUBU [Tyr-D-Ser(OtBu)-Gly-Phe-Leu-Thr(OtBu)] (Ki delta = 4.68 nM; Ki mu = 475 nM) or a loss of affinity for DTTBULET [Tyr-D-Thr(OtBu)-Gly-Phe-Leu-Thr] (Ki delta = 866 nM; Ki mu = 4500 nM).