It is known that the electronic transport and heat conduction of thermoelectric materials are very sensitive to structural changes. In this article, the effect of Ag substitution on the crystal structure and hence thermoelectric properties of Cu 1−x Ag x InTe 2 (x = 0, 0.05, 0.15, 0.25, 0.50, 0.75, and 1.00) solid solutions are investigated. The structural analysis shows that with the increasing Ag content, the lattice strain changes from tensile stress to compressive stress, and the tetrahedral distortion first relieves and then aggravates, which influences not only electronic but also thermal transport properties. The replacement of Cu by Ag results in the reduction of carrier concentration and lattice thermal conductivity. Although the enhancement in zT values of Cu 1−x Ag x InTe 2 samples mainly originates from the significantly reduced lattice thermal conductivity, the improved electronic transport properties due to Ag substitution also play an important role. As a result, a maximum zT value of ∼1.36 is achieved for Cu 0.75 Ag 0.25 InTe 2 at 823 K, which is a 92% improvement compared with the value of pristine CuInTe 2 . Our study provides a primary view of the relationship between the structure and thermoelectric performance, which is beneficial to the optimization of thermoelectric properties.

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Twenty propylene and butylene tethered di-isatin heteronuclear compounds 5a-t were synthesized, and their antibacterial activities were evaluated. Most of the synthesized di-isatin heteronuclear derivatives were active against both Gram-positive and Gram-negative strains, and some of them exhibited considerable activities against drug-resistant organisms. In particular, di-isatin 5a (MIC: 32-512 μg/mL) was more active than the reference vancomycin against Gram-negative pathogens, demonstrating the antibacterial potential of diisatin heteronuclear compounds. The inhibitory activity of di-isatin 5a was higher than mono-isatin against Escherichia coli DNA gyrase, suggesting the dimers could improve the inhibitory activity against DNA gyrase when compared with the isatin. The structure-activity relationship was discussed to provide an insight for rational designs of more efficient antibacterial candidates.

A series of novel moxifloxacin/gatifloxacin‐1,2,3‐triazole‐isatin hybrids (8a–i) were designed, synthesized, and screened for their in vitro anticancer activity in this paper. All of the synthesized hybrids were active against A549 and HepG2 cancer cell lines, whereas the parent drugs moxifloxacin and gatifloxacin were devoid of activity. Among them, hybrid 8i (IC50: 41.1–98.3 μM) showed considerable activity against A549, HepG2, and MCF‐7 cancer cell lines, and it was no inferior to Vorinostat (IC50: 64.32 to >100 μM) against the three cancer cell lines. Thus, this kind of hybrids has potentiality for discovery of new anticancer candidates for clinical deployment in the control and eradication of cancers.

Background: Methicillin-resistant S. aureus (MRSA) has already tormented humanity and the environment for a long time and is responsible for many difficult-to-treat infections. Unfortunately, there are limited therapeutic options, and MRSA isolates with complete resistance to vancomycin, the first-line drug for the treatment of MRSA infections, have already emerged in recent years. Moxifloxacin retained activity against mutant bacterial strains with various levels of fluoroquinolones resistance and had a lower potential to select for resistant mutants. Isatin is a versatile structure, and its derivatives are potent inhibitors of many enzymes and receptors. The fluoroquinolone-isatin derivatives demonstrated excellent antibacterial activity against both drug-sensitive and drug-resistant organisms. The structure-activity relationship elucidated that incorporation of 1,2,3-triazole moiety into the C-7 position of fluoroquinolone skeleton was favorable to the antibacterial activity. Accordingly, fluoroquinolone derivatives with isatin and 1,2,3-triazole fragments at the side chain on the C-7 position are promising candidates to fight against drug-resistant bacteria. Objective: To explore more active moxifloxacin derivatives to fight against MRSA and enrich the structure-activity relationships. Methods: The synthesized moxifloxacin derivatives 7a-i and 14a-f were evaluated for their antibacterial activity against a panel of MRSA strains by means of standard two-fold serial dilution method. Results: The majority of the synthesized moxifloxacin derivatives were active against most of the tested MRSA strains with MIC values in a range of 1 to 64 μg/mL. The mechanistic investigations revealed that topoisomerase IV was one of the targets for antibacterial activity. Conclusion: These derivatives are useful scaffolds for the development of novel topoisomerase IV inhibitors.