Exploring the synthetic potency of the first furanothioglycoligase through original remote activation.

Thioglycosidic bonds are of utmost importance in biomolecules as their incorporation led to more stable glycomimetics with potential drug activities. Until now only chemical methods were available for their incorporation into glycofuranosyl conjugates. Herein, we wish to describe the use of the first furanothioglycoligase for the preparation of a great variety of thioaryl derivatives with moderate to excellent yields.

From molecule to sexual behavior: the role of the neuropentapeptide proctolin in acoustic communication in the male grasshopper Chorthippus biguttulus.

Acoustic communication in male Chorthippus biguttulus is a suitable behavioral model to explore the physiological effects and underlying molecular mechanisms of identified neuropeptides. Proctolin plays a modulatory role in a neuronal circuit controlling sexual behavior in these insects. Activation of proctolin receptors triggers courtship singing (the second level of excitation in sexual behavior) that is preceded by call singing triggered by muscarinic acetylcholine receptor activation.

Synthesis and characterization of new galanthamine derivatives comprising peptide moiety.

New analogues of galanthamine containing peptide fragments either at 6 or 11 position, were synthesized by reaction between galanthamine molecule and dipeptides and tripeptide, derivatives of N-(3,4-dichlorophenyl)-D,L-Ala-OH. The best results according to yields, easily purification of the target products, and simplicity of the scheme realisation was achieved by using of cyanomethyl ester of Boc-Gly-OH as activated compound.

Synthesis of two peptide mimetics as markers for chemical changes of wool's keratin during skin unhairing process.

The sheep skins unhairing process with preliminary alkaline treatment of the wool leads to two unnatural dipeptide mimetics lysinoalanine (Lys(*) - Ala) and ornithinoalanine (Orn(*)- Ala) obtaining. They are result from the keratin hydrolysis process. The changes of wool keratin make it resistant to sulphide degradation.

Investigation of kinetic parameters in vitro of serine proteinases included in the blood coagulation cascade.

During the last years the cases and death due to hemostatic violations exceed that of tumors. Enormous efforts have devoted to the prevention and treatment of some diseases such as arterial thrombosis. Antistasin, a 15 kDa anticoagulant protein isolated from salivary glands of the Mexican leech Haementeria officinalis, has been shown to be a potent inhibitor of Factor Xa in the blood coagulation cascade.

Synthesis and structure-activity relationship of new analogues of antistasin.

Intensive investigation connected with the development of new anticoagulant agents for the treatment of cardiovascular diseases was carried out. Direct and specific inhibition of thrombin and Factor Xa-like serine proteases in the coagulation cascade has been the focus of many efforts to design novel anticoagulants over the past decade. This work reports the synthesis and biological activity of new anticoagulant peptide analogues of natural isoforms 2 and 3 of antistasin.