The ring expansion of cyclopropane derivatives provides a powerful method to construct synthetically useful four-membered carbocycles. Herein, a new type of gold(I)-catalyzed ring expansion of an unactivated alkynylcyclopropane/sulfonamide trapping strategy to (E)-2-alkylidenecyclobutanamines was described. The reaction tolerates a range of aryl and alkyl substituents with moderate to good yields.

Simple hydroxamic acids (XHA) are hydrophilic organic compoundswith the general formula RCONHOH that can act as O,O donor ligands with high affinities for hard cations such as Fe3+, Np4+ and Pu4+ with which they form 5-membered chelate rings (Muri et al.,2002; Desaraju & Winston,1986; Carrott et al.,2007). They have a wide range of applications in many fields, including as enzyme inhibitors, so...

Histone deacetylase inhibitors (HDACi) target abnormal epigenetic states associated with a variety of pathologies, including cancer. Here, the development of a prodrug of the canonical broad-spectrum HDACi suberoylanilide hydroxamic acid (SAHA) is described. Although hydroxamic acids are utilized universally in the development of metalloenzyme inhibitors, they are considered to be poor pharmaco...

LpxC inhibitors represent a promising class of novel antibiotics selectively combating Gram-negative bacteria. In chiral pool syntheses starting from D- and L-xylose, series four 2r,3c,4t-configured C-furanosidic was obtained. The synthesized hydroxamic acids were tested for antibacterial inhibitory activity, the acquired biological data compared with those previously C-furanosides, molecular d...

In this work, we present the synthesis and anti-trypanosomal activity of 2-(4-(adamant-1-yl)phenyl)-N-hydroxyarylamides, 1a,b 2-(4-(adamant-1-yl)phenoxy)-N-hydroxyacetamide, 1c. The 4-(adamant-1-yl)phenyl- 4-(adamant-1-yl)phenoxy- moieties, which are endowed with promising drug-like properties, functionalized at side chain termini as hydroxamic acids. phenoxy acetohydroxamic derivative, 1c, sho...

Motivation. Substituted 1,3,5-triazines are known as useful herbicidal substances. In view of reducing the cost of biological screening, computational methods are carried out for evaluating the biological activity of organic compounds. Often a class of bioactives differ only in the substituent attached to a basic skeleton. In such cases substituent descriptors will give the same prospecting res...

High throughput screening (HTS) of a 205 member Schiff base salicylaldimine ligand library derived from salicylaldehydes bearing bulky ortho-substituents, i.e., 9-anthracenyl, 1,4,5,8-tetramethylanthracenyl or triptycenyl, reacted in-situ with (p-tolyl)CrCl2(thf)3, identified two new classes of highly active chromium based systems for the oligomerization and polymerization of ethylene, respecti...

Chiral mixed phosphorus/sulfur ligands 1-3 have been shown to be effective in enantioselective Rh-catalyzed dehydroamino acid hydrogenation and ketone hydrosilylation reactions (eqs 1, 2). After assaying the influence of the substituents at sulfur, the substituents on the ligand backbone, the relative stereochemistry within the ligand backbone, and the substituents at phosphorus, ligands 2c (R ...

Cyclic hydroxamic acid glucosides are present at high concentrations immediately after germination in wheat (Triticum aestivum L.). Changes in the activity of UDP-Glucose:cyclic hydroxamic acid glucosyltransferase (EC 2.4.1.-) in wheat were investigated using the cyclic hydroxamic acids 2.4-dihydroxy-1,4-benzoxazin-3-one (DIBOA) and its 7-methoxy derivative (DIMBOA) as sugar acceptors. Glucosyl...

A spectrophotometric method is used to determine the acidity constants of some derivatives of 9,10-anthraquinone in binary methanol-water mixtures at 25 °C. There is a linear inverse relationship between pKa of all acids and the mole fraction of methanol in the mixed solvent. The influence of substituents in the molecular structure on the ionization constants is discussed.