Despite their high efficacy NSAIDs have significant side effects due to non-selective inhibition of COX-1 and COX-2. Due this, medical chemists still pay considerable attention design synthesis, in particular the creation hybrid molecules that combine structure a fragment with anti-inflammatory activity quinazoline heterocycle.
 The aim present study is develop methods for synthesis [1,2,4...

Functionalized acyclic and cyclic guanidines have a wide range of biological activity. In particular, they possess antitumor, antibacterial activities, are immunosuppressants, anesthetics, analgesics analogues natural alkaloids. The search methods for the synthesis new guanidine derivatives is an urgent problem.
 introduction unsaturated alkyl substituent to backbone opens way heterocyclic...

Nonribosomal peptide synthetases (NRPSs) are a family of multidomain, multimodule enzymes that synthesize structurally and functionally diverse peptides, many of which are of great therapeutic or commercial value. The central chemical step of peptide synthesis is amide bond formation, which is typically catalyzed by the condensation (C) domain. In many NRPS modules, the C domain is replaced by ...

A novel synthetic methodology has been developed for the synthesis of dihydro-β-carboline derivatives employing oxidative amidation-Bischler-Napieralski reaction conditions using tryptamine and 2,2-dibromo-1-phenylethanone as key starting materials. A number of dihydro-β-carboline derivatives have been synthesized in moderate to good yields using this methodology. Attempts were made towards the...

BACKGROUND Virulence in the pathogenic bacterium Yersinia pestis, causative agent of bubonic plague, has been correlated with the biosynthesis and transport of an iron-chelating siderophore, yersiniabactin, which is induced under iron-starvation conditions. Initial DNA sequencing suggested that this system is highly conserved among the pathogenic Yersinia. Yersiniabactin contains a phenolic gro...

Rhodacyclopentanones derived from carbonylative C-C activation of cyclopropyl ureas can be "captured" by pendant nucleophiles prior to "collapse" to 1,3-diazepanes. The choice of N-substituent on the cyclopropane unit controls the oxidation level of the product, such that C4-C5 unsaturated or saturated systems can be accessed selectively.