Since 2000, when the histamine H4 receptor (H4R) was cloned, it has constituted an interesting target for drug development. Pharmacological studies suggest the potential utility of histamine H4R antagonists/inverse agonists in the treatment of inflammatory diseases, e.g. allergic rhinitis, asthma, atopic dermatitis, colitis, or pruritus. The first H4R ligands were non-selective compounds, but i...

Abstract Derivatives of fused 1,2,4-triazines containing heterocyclic and metallocene fragments were obtained by one-pot oxidative cyclization hydrazones in the presence hypervalent iodine(III) reagents. For 1,2,4-triazolo[4,3-a]azines, ability to activate HSF1 was investigated. The compounds shown increase degree activation. It that can be used induce Hsp70 expression decrease extent mutant HT...

C–H borylation of N-heteroarenes is an efficient yet highly challenging route to borylated aromatics. In a recent issue Nature, Leonori and co-workers demonstrated novel strategy toward this end by utilizing boryl-radical-based Minisci-type reaction that shows orthogonal site selectivity transition-metal-catalyzed approaches. Direct aromatic bonds straightforward means accessing diverse arene s...

2-Amino-3-functionally substituted thiophene de­ rivatives are important intermediates to the phar­ maceutically important thieno[2,3-d]pyrimidines [2]. These thiophene derivatives were available from the procedures published by K. Gewald [3, 4] via either the reaction of a-methylene ketones with active methylene nitriles in presence of elementary sulphur of from a-mercaptoketones and active me...

Light-induced cyclization of several substituted 2-(2-fluorophenylazo)azines in the presence of Ca(2+) ions to the corresponding triazinium derivatives is investigated experimentally and computationally. The azo derivatives of 4-methylpyridine 4 undergo facile cyclization to the corresponding triazinium 1, and the rate of cyclization increases with increasing number of fluorine atoms at the ben...