Synthesis of Calix[4]arene-Based Porous Organic Cages and Their Gas Adsorption.

Two crystalline large-sized porous organic cages (POCs) based on conical calix[4]arene (C4A) were designed and synthesized. The four-jaw C4A unit tends to follow the face-directed self-assembly law with the planar triangular building blocks such as tris(4-aminophenyl)amine (TAPA) or 1,3,5-tris(4-aminophenyl)benzene (TAPB) to generate a predictable cage with a stoichiometry of [6+8]. The formation of the large cages is confirmed through their relative molecular mass measured using MALDI-TOF/TOF spectra.

Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-]indole Derivatives Against Gram-Negative Multidrug-Resistant Pathogens.

Due to the poor permeability across Gram-negative bacterial membranes and the troublesome bacterial efflux mechanism, only a few GyrB/ParE inhibitors with potent activity against Gram-negative pathogens have been reported. Among them, pyrimido[4,5-]indole derivatives represented by GP-1 demonstrated excellent broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria but were limited by hERG inhibition and poor pharmacokinetics profile. To improve their drug-like properties, we designed a series of novel pyrimido[4,5-]indole derivatives based on the tricyclic scaffold of GP-1 and the C-7 moiety of acorafloxacin.

Recent advances in antibacterial agents.

Antimicrobial resistance is a global challenge and the effectiveness of old antibiotics is decreasing. Discovery and development of antibacterial agents have been accelerated to replenish the arsenal of antibiotics which is limited and shrinking. In recent years, significant advances have achieved in the antibacterial area, including new compounds of known classes and new compounds with new mechanisms.

Chemistry and biology of glycopeptides with antibiotic activity.

Glycopeptides with potent antibiotic activity are vital for the treatment of severe infections that caused by Gram-positive bacteria, especially methicillin-resistant Staphylococcus aureus. Recently, the glycopeptide-resistant Grampositive bacteria present a serious challenge to public health after more than decades of clinical use. Additionally, the antibacterial activity and side effect become an increasing crisis and should have to be taken into account.