Tuberculosis still remains one of the most common, communicable, and leading deadliest diseases known to mankind throughout the world. Drug-resistance in Mycobacterium tuberculosis which threatens to worsen the global tuberculosis epidemic has caused great concern in recent years. To overcome the resistance, the development of new drugs with novel mechanisms of actions is of great importance. Imidazole-containing derivatives endow with various biological properties, and some of them demonstrated excellent anti-tubercular activity. As the most emblematic example, 4-nitroimidazole delamanid has already received approval for treatment of multidrug-resistant tuberculosis infected patients. Thus, imidazole-containing derivatives have caused great interests in discovery of new anti-tubercular agents. Numerous of imidazole-containing derivatives were synthesized and screened for their in vitro and in vivo anti-mycobacterial activities against both drug-sensitive and drug-resistant Mycobacterium tuberculosis pathogens. This review aims to outline the recent advances of imidazole-containing derivatives as anti-tubercular agents, and summarize the structure-activity relationship of these derivatives. The enriched structure-activity relationship may pave the way for the further rational development of imidazole-containing derivatives as anti-tubercular agents.

Inorganic semiconductor nanoparticles, such as CdSe quantum dots, are considered to be a promising alternative to fullerene derivates for application as electron acceptors in polymer-based bulk heterojunction solar cells. The main potential advantage is the strong light absorption of CdSe nanoparticles with a spectral bandwidth, which can even be tuned, due to the quantum size effect. However, the impact of the particle size on the performance of polymer/CdSe solar cells has remained largely unexplored so far. Therefore, the influence of particle size in hybrid solar cells using a blend of poly(3-hexylthiophene) (P3HT) and quasi-spherical CdSe nanoparticles on relevant cell parameters and the overall solar cell performance is systematically studied in the present work. As the most important result, an increase of the open-circuit voltage (VOC) can be found for smaller nanoparticles and can be explained by an “effective bandgap” model. In contrast, no significant changes of the short-circuit current density with particle size are observed. Smaller particles were found to yield a lower fill factor, compensating the gain in VOC, so that the power conversion efficiency finally turned out to be independent of the particle size in this study. Spectral differences observed in the respective external quantum efficiency spectra of the solar cells can be attributed to size-dependent changes of the particle absorption. Temperature-dependent measurements of the current-voltage (I-V) characteristics suggest that the transport of photogenerated charge carriers in the bulk heterojunction is limited by localized states, with activation energy beyond thermal energy at room temperature.

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N -Nitrosonornicotine (NNN) is a human carcinogen present in cigarette smoke and smokeless tobacco. Urinary NNN is usually measured in order to assess the exposure to this toxicant for tobacco users. NNN excretion in urine can be highly biased due to the formation of NNN by nitrosation of nornicotine under acidic conditions, both endogenously and exogenously. Hence, urinary NNN levels may not necessarily correctly reflect the product-specific exposure. Measurement of plasma NNN may be less prone to endogenous formation due to the stable pH (7.4) of blood. We developed an LC–MS/MS method for the quantification of NNN using 1 mL of human plasma. Validation according to FDA guidelines proved that the method is selective and highly sensitive with an LLOQ of 0.3 pg/mL. Accuracy and precision averaged to 98.7 and 7.5% (CV), respectively. The assay was applied to plasma samples collected from 10 experienced moist smokeless tobacco users during and after a single use of 2 g of the product for 40 min under controlled use conditions. Blood was drawn at 15 time points over a 6 h time course. The maximum NNN concentration ( C max ) ranged from 3.5 to 10 pg/mL (mean: 7.1 pg/mL) at a t max of 32 min. Plasma NNN and nicotine were found to have similar time courses. In conclusion, the determination of NNN in plasma may be fit-for-purpose to evaluate the product-use-specific exposure to this carcinogen.

The resistance index of hybrid 8i was 1, indicating that hybrid 8i has no cross-resistance with the first-line anti-TB agent. Thus, hybrid 8i could act as a lead for further optimization.

Pyrazolopyrimidinone compounds are widely found in nature. Since the first pyrazolopyrimidinone was synthesized in 1888, synthesis and application of pyrazolopyrimidinones have been more and more active. Some pyrazolopyrimidinones are applied to the treatment of commom diseases, and are called the crown jewels in drug discovery history. For more than one century, various synthetic methodologies concerning pyrazolopyrimidinone have been developed. However, no specific review about pyrazolopyrimidinones was present. This review comments the synthesis of pyrazolopyrimidinone from the point of view of the synthetic methodology.

Tobacco-specific nitrosamine (TSNA) formation occurred during aerosol generation from select commercial cig-a-like e-cigarette products. To understand the drivers behind the potential formation of TSNAs in electronic cigarette (e-cigarette) aerosols and e-liquids, model e-liquid systems were generated in the lab to demonstrate that nitrite can react with nicotine and minor alkaloids to form TSNAs in e-liquids. In the presence of nitrite and nicotine, TSNA levels in e-liquids increased over time and the process was accelerated by elevated temperature. Additionally, TSNAs formed during aerosol generation when nitrite was present in the corresponding e-liquids. The commercial e-cigarette products that showed higher levels and formation of TSNAs were observed to contain nitrite and minor alkaloid impurities in the corresponding e-liquids. This study provides valuable information about drivers for TSNA formation in e-liquids and e-cigarette aerosols that may be applied to the evaluation and quality assurance of e-cigarette products.

In view of the important role of quinazoline skeletons in anti-cancer drugs like Gefitinib  and the vital importance of organoselenium compounds in biomedicine field, in this protocol, twenty quinazoline selenium derivatives were designed and synthesized with the aim to develop new anti-cancer drugs by utilizing the synergistic effects of quinazoline skeleton and selenium. In addition, the synthetic method of thioether substituted quinazolines was improved. The biological activities of title compounds were determined against A549 cancer cells in vitro by using MTT assay at 1 μM and 10 μM concentrations. The results showed that most of the title compounds had good anticancer activities. Of note, 6-chloro-4-benzylselenoquinazoline (G5) exhibited better inhibitory activity (67.8% inhibition ratio) than the positive control drug Gefitinib  (62.9% inhibition ratio) at the concentration of 10 μM. These findings will provide some clues for further research of anticancer drugs.