Ciprofloxacin derivatives and their antibacterial activities.

Bacterial infections represent a significant health threat globally, and are responsible for the majority of hospital-acquired infections, leading to extensive mortality and burden on global healthcare systems. The second generation fluoroquinolone ciprofloxacin which exhibits excellent antimicrobial activity and pharmacokinetic properties as well as few side effects is introduced into clinical practice for the treatment of various bacterial infections for around 3 decades. The emergency and widely spread of drug-resistant pathogens making ciprofloxacin more and more ineffective, so it's imperative to develop novel antibacterials. Numerous of ciprofloxacin derivatives have been synthesized for seeking for new antibacterials, and some of them exhibited promising potency. This review aims to summarize the recent advances made towards the discovery of ciprofloxacin derivatives as antibacterial agents and the structure-activity relationship of these derivatives was also discussed.

4-Quinolone derivatives and their activities against Gram positive pathogens.

Gram-positive bacteria are responsible for a broad range of infectious diseases, and the emergency and wide spread of drug-resistant Gram-positive pathogens including MRSA and MRSE has caused great concern throughout the world. 4-Quinolones which are exemplified by fluoroquinolones are mainstays of chemotherapy against various bacterial infections including Gram-positive pathogen infections, and their value and role in the treatment of bacterial infections continues to expand. However, the resistance of Gram-positive organisms to 4-quinolones develops rapidly and spreads widely, making them more and more ineffective. To overcome the resistance and reduce the toxicity, numerous of 4-quinolone derivatives were synthesized and screened for their in vitro and in vivo activities against Gram-positive pathogens, and some of them exhibited excellent potency. This review aims to outlines the recent advances made towards the discovery of 4-quinolone-based derivatives as anti-Gram-positive pathogens agents and the critical aspects of design as well as the structure-activity relationship of these derivatives. The enriched SAR paves the way to the further rational development of 4-quinolones with a unique mechanism of action different from that of the currently used drugs to overcome the resistance, well-tolerated and low toxic profiles.

Molecular weight dependence of hybrid shish kebab structure in injection molded bar of polyethylene/inorganic whisker composites.

In our previous work, a hybrid shish kebab structure, with polyethylene (PE) crystal lamellae periodically decorated on the surface of an inorganic whisker (SMCW) and aligned approximately perpendicular to the long axis of the whisker, has been observed in the injection molded bar of PE/SMCW composites. To investigate the effect of the molecular weight of the PE matrix on the formation of the hybrid shish kebab structure and the corresponding physical properties of HDPE/SMCW composites, in this work, three types of PE with different molecular weights were used to prepare the composites. They were first melt blended and then subjected to dynamic packing injection molding (DPIM), in which the prolonged shear was exerted on the melt during the solidification stage. An obvious hybrid shish kebab (HSK) structure, with PE crystal lamellae closely packed on the surface of the SMCW, was found in the samples with a low molecular weight PE (LMW-PE) matrix and a medium molecular weight PE (MMW-PE) matrix. However, in samples with a high molecular weight PE (HMW-PE) matrix, an incomplete HSK structure with PE crystal lamellae loosely decorated on the surface of the SMCW was observed. Furthermore, DSC results indicated that SMCW served as a good nucleating agent only for the composite with a LMW-PE matrix and the nucleation efficiency decreased with increasing PE molecular weight. Correspondingly, the tensile strength of the PE/SMCW composites was significantly improved by adding SMCW for the samples with a LMW-PE or MMW-PE matrix. Especially for samples with a LMW-PE matrix, the tensile strength was remarkably enhanced by the presence of only 1 wt % SMCW. For the composites with a HMW-PE matrix, the addition of SMCW had almost no reinforcing effect on the composites. The molecular weight dependence of the formation of HSK and property enhancement was discussed on the basis of the chain mobility and crystallization capability of the PE matrix.