Design, synthesis and antimicrobial activity evaluation of novel Marinoquinoline derivatives against phytopathogenic bacteria.

Background: Plant diseases caused by plant pathogens pose a great threat to biodiversity and food security, and the problem of drug resistance caused by traditional antibiotics and fungicides is becoming more and more serious. It is urgent to develop new antibacterial molecules with low toxicity and high efficiency. Marinoquinoline A is an alkaloid isolated from marine actinomycetes and has a variety of pharmacological activities.

Design, Synthesis, and Biological Evaluation of Novel Quinoline Derivatives against Phytopathogenic Bacteria Inspired from Natural Quinine Alkaloids.

A series of 2-(trifluoromethyl)-4-hydroxyquinoline derivatives were designed and synthesized with introduction of the antibacterial fragment amino alcohols, and their antibacterial activity against plant phytopathogenic bacteria was evaluated for the development of quinoline bactericides. It is worth noting that compound exhibited excellent antibacterial activity with a minimum inhibitory concentration (MIC) value of 3.12 μg/mL against ().

Design, Synthesis, and Antimicrobial Activity Evaluation of Novel Isocryptolepine Derivatives against Phytopathogenic Fungi and Bacteria.

This research adopted the Fischer indole synthesis method to continue constructing a novel drug-like chemical entity based on the guidance of isocryptolepine and obtained four series of derivatives: , , , and . The antimicrobial activity of these derivatives against plant pathogens was further evaluated. The results showed that had the best antifungal effect against , and its EC value was up to μg/mL.

TPGS-b-PBAE Copolymer-Based Polyplex Nanoparticles for Gene Delivery and Transfection In Vivo and In Vitro.

Poly (β-amino ester) (PBAE) is an exceptional non-viral vector that is widely used in gene delivery, owing to its exceptional biocompatibility, easy synthesis, and cost-effectiveness. However, it carries a high surface positive charge that may cause cytotoxicity. Therefore, hydrophilic d-α-tocopherol polyethylene glycol succinate (TPGS) was copolymerised with PBAE to increase the biocompatibility and to decrease the potential cytotoxicity of the cationic polymer-DNA plasmid polyplex nanoparticles (NPs) formed through electrostatic forces between the polymer and DNA.

A new protein-ligand binding sites prediction method based on the integration of protein sequence conservation information.

Background: Prediction of protein-ligand binding sites is an important issue for protein function annotation and structure-based drug design. Nowadays, although many computational methods for ligand-binding prediction have been developed, there is still a demanding to improve the prediction accuracy and efficiency. In addition, most of these methods are purely geometry-based, if the prediction methods improvement could be succeeded by integrating physicochemical or sequence properties of protein-ligand binding, it may also be more helpful to address the biological question in such studies.