The diazabicyclooctane (DBO) scaffold is the backbone of non-β-lactam-based second generation β-lactamase inhibitors. As part our efforts, we have synthesized a series DBO derivatives A1 – 23 containing amidine substituents at C2 position bicyclic ring. These compounds, alone and in combination with meropenem, were tested against ten bacterial strains for their antibacterial activity vitro. All...

The key step in the synthesis of the 7,9-diazabicyclo[4.2.2]decane system was a modified Dieckmann condensation of piperazinebutyrate 11, which makes use of trapping the first cyclized intermediate with TMS-Cl. Reduction of the bicyclic ketone 14 with LiBH(4) at -90 °C provided diastereoselectively (>99 : 1) the syn-configured alcohol 15a, which was converted into the final alcohol and ethers 1...

Introduction: The chemistry of metal complexes derived from heterocyclic compounds has attracted considerable interest due to the broad range of pharmacological activities of such compounds. The important pathogens such as Escherichia coli, and Staphylococcus aureus are wildly caused many diseases. So antibacterial activity of Zn (Ⅱ), Ni (Ⅱ), Co (Ⅱ) and Cu (Ⅱ) chromone complexes against two kin...

The catalytic decarboxylation of aromatic carboxylic acids provides an alternative route to generate aryl metal species in situ without using organometallic compounds. Herein, a cationic iridium-catalyzed through CO2 extrusion is described. substrate scope broad, and the reaction proceeds even presence various functional groups. Additionally, potential utility was demonstrated decarboxylative h...

Cancerous cells have an acutely increased demand for energy, leading to increased levels of human glucose transporter 1 (hGLUT1). This up-regulation suggests hGLUT1 as a target for therapeutic inhibitors addressing a multitude of cancer types. Here, we present three inhibitor-bound, inward-open structures of WT-hGLUT1 crystallized with three different inhibitors: cytochalasin B, a nine-membered...

Seven norsesterterpene peroxides: epimuqubilin A (1), muqubilone B (2), unnamed cyclic peroxide ester (3), epimuqubilin B (4), sigmosceptrellin A methyl ester (5), sigmosceptrellin A (6), and sigmosceptrellin B methyl ester (7), isolated from the marine sponge Latrunculia sp., were examined with regard to their effects on nitric oxide (NO) production in lipopolysaccharide (LPS)-activated murine...

ligands derived from 8-quinoline, 6-quinoline, 1 -isoquinoline, and 5-isoquinoline were synthesized. these compounds have been used as ligands for complexation of transition metals, such as copper(ii) and nickel(ii). according to the spectrosocopic data, copper(ii) cation forms (i: 1) and (i:2) complexes with 2-(8-quinoly1)-l,l,3,3- tetramethylguanidine and 2- (i '-isoquinoly1)- 1,1,3,3-te...

Quinolones are a very important family of antibacterial agents that are widely prescribed for the treatment of infections in humans. Since their discovery in the early 1960s, the quinolone group of antibacterials has generated considerable clinical and scientific interest. Two major groups of compounds have been developed from the basic molecule: quinolones and naphthyridones. The 4-pyridone-3-...