Human neutrophil elastase (HNE) is a potent serine protease belonging to the chymotrypsin family and is involved in a variety of pathologies affecting the respiratory system. Thus, compounds able to inhibit HNE proteolytic activity could represent effective therapeutics. We present here the synthesis of new thiazol-2-(3H)-ones as an elaboration of potent HNE inhibitors with an isoxazol-5-(2H)-o...

The Schiff base reaction and aldol condensation that occur during sample preparation can lead to the reduction of aldehyde content in the analysis of traditional Korean rice wine, makgeolli. The contents of aldehydes were decreased, whereas those of hydroxy carbonyl compounds were increased by increasing the pH. In the presence of added amino acids, the levels of aldehydes in makgeolli were red...

The title compound, C(29)H(28)O(9), was isolated from the reaction of 4,6-dimeth-oxy-2-(4-methoxy-phen-yl)-3-benzofuran and α-methoxy-carbonyl-cinnaminate. The two aromatic rings form a dihedral angle of 22.7 (1)°. One methoxy-carbonyl group is disordered between two orientations in a 0.612 (4):0.388 (4) ratio. The crystal structure exhibits no significantly short inter-molecular contacts.

The first mercury-catalyzed synthesis of 1,2-diketones by alkyne oxidation has been developed. This inexpensive method extends the potential mercury catalysis and allows rapid construction various α-carbonyl amides in good yields with high functional group tolerance.

[structure: see text] Pyridoxamine is known to be an effective inhibitor of both advanced glycation (AGE) and advanced lipoxidation (ALE) end products. The synthesis of a novel multifunctional AGE and ALE inhibitor, 6-dimethylaminopyridoxamine (dmaPM, 11) is described. The 6-dimethylamino substituent increases the radical trapping ability of pyridoxamine's phenolic group. Results obtained durin...

The reaction between bis(2-benzothiazolyl)ketone and vinyl Grignard reagents bearing different substituents on the vinyl moiety gave the product derived from attack on the carbonylic carbon- and/or oxygen-atom. The regioselectivity of the attack depends on the kind of substituents bound to the vinylic carbon atoms and on their relative position. The reaction between vinylmagnesium bromide and 2...

Entomopathogenic fungi seem to be interesting as a source of biologically active compounds such as an insecticides1) and immunosuppressants2,3), because all insect orders are susceptible to fungal diseases. With the goal of finding novel bioactive compounds from fungi, we investigated metabolite diversity using an HPLC screening program. During the screening process, we isolated two novel metab...

In the title compound, C(22)H(17)BrN(2)O(4)S, the central dihydropyrimidine ring, with a chiral C atom, is significantly puckered and adopts a half-chair conformation with the chiral C atom displaced from the mean plane of the remaining ring atoms by 0.305 (6) Å. The hydroxy-phenyl ring is positioned axially to the pyrimidine ring and almost bisects it, the dihedral angle between the mean-plane...