A series of novel guanidine derivatives were synthesized in three steps and their anti-inflammatory activities in vitro and in vivo evaluated. 2-Aminopyridin-3-ol (1) was reacted with thiophosphoryl chloride (2) to give a monochloride (3). It was further reacted with cyanamide to afford the corresponding cyanamine (4), which was subsequently reacted with different heterocyclic amines to form th...

Former p~pers from this laboratory indicate that the penetration of a weak base, ammonia,* and of a strong base, guanidine, 2 is probably preceded by a chemical reaction with a constituent of the protoplasm. On the other hand the penetration of a weak acid, hydrogen sulfide, s appears to take place by simple diffusion of molecular hydrogen sulfide through the non-aqueous protoplasm. What is the...

Batzelladine C (3) is a tricyclic guanidine alkaloid of unknown stereochemistry at one centre as well as unknown absolute stereochemistry. The two possible diastereoisomers of the methyl ester corresponding to this compound have been synthesised, permitting the relative and absolute stereochemistry of this compound to be assigned.

A novel 2',4'-BNA/LNA analog bridged by guanidine, termed as guanidine bridged nucleic acid (GuNA), was synthesized and incorporated into oligonucleotides. Thermal stabilities and nuclease resistance of GuNA-modified oligonucleotides were investigated and compared with those of 2',4'-BNA/LNA and natural DNA oligonucleotides. GuNA exhibited interestingly high binding affinity towards complementa...

Although electrostatic interactions contribute only a part of the interaction energies between macromolecules, unlike dispersion forces they are highly directional and therefore dominate the nature of molecular packing in crystals and in biological complexes and contribute significantly to differences in inhibition strength among related enzyme inhibitors. In the reported study, a wide range of...

Analytical methods based on spectroscopic techniques were developed and validated for the determination of diethyl phthalate (DEP) and polyhexamethylene guanidine (PHMG), which may occur in unrecorded alcohol. Analysis for PHMG was based on UV-VIS spectrophotometry after derivatization with Eosin Y and (1)H NMR spectroscopy of the DMSO extract. Analysis of DEP was performed with direct UV-VIS a...

In studies on muscular dystrophy in young individuals investigations of the urine were made along three lines, as follows: (a) the estimation of creatinine and creatine, according to Folin (1) and Benedict (2) respectively; (b) the study as to whether the creatine findings include other substances than creatine; (c) the possibility that in muscular dystrophy guanidine intoxication plays a promi...

Contributions of tyrosyl residues to trypsinand chymotrypsin-inhibitory activities in two homologous proteinase inhibitors were investigated by modifying them with N-acetylimidazole under various conditions. In Bowman-Birk soybean proteinase inhibitor, Tyr 55, immediately following the antichymotryptic site, Leu 53-Ser 54, is relatively inaccessible to N-acetylimidazole and can only be acetylat...