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.

Study on anti-atherosclerotic effect of Suxiao Jiuxin Pill and its mechanism.

BACKGROUND: Suxiao Jiuxin Pill is composed of Ligusticum wallichii, Borneolum Syntheticum and other drugs; it has qi promoting and blood circulation activating, meridian dredging and pain relieving efficacies. The objective of this paper is to study the effect of Suxiao Jiuxin Pill (quick-acting heart reliever), in atherosclerosis (AS) rat model and explore the mechanism for its prevention and treatment of AS. MATERIALS AND METHODS: AS rat model was established by high cholesterol diet and single intra-peritoneal injection of increased dose of vitamin D3. RESULTS: Compared with the model group, Suxiao Jiuxin Pill medium-and high-dose groups and atorvastatin group can effectively regulate lipid metabolism. CONCLUSION: We conclude that Suxiao Jiuxin Pill has a good hypo-lipidemic effect, and can inhibit the occurrence and development of AS.

3-(2-Hydroxy-ethyl)-2-(p-tolyl-amino)-quinazolin-4(3H)-one.

In the title compound, C(17)H(17)N(3)O(2), the quinazolinone ring system is essentially planar. The benzene ring is twisted with respect to it by a dihedral angle of 32.7 (5)°. The mol-ecular conformation is stabilized by an N-H⋯O hydrogen bond, and the crystal structure is stabilized by inter-molecular O-H⋯N inter-actions.