The growing prevalence of microbial infections, and antimicrobial resistance (AMR) stemming from the overuse and misuse of antibiotics, call for novel therapeutic agents, particularly ones targeting resistant microbial strains. Scientists are striving to develop innovative agents to tackle the rising microbial infections and abate the risk of AMR. Pyrazole, a five-membered heterocyclic compound belonging to the azole family, is a versatile scaffold and serves as a core structure in many drugs with antimicrobial and other therapeutic effects. In this review, we have updated pyrazole-based antibacterial and antifungal agents mainly developed between 2016 and 2024, by combining with diverse pharmacophores such as coumarin, thiazole, oxadiazole, isoxazole, indole, etc. Meanwhile, the various strategies (molecular hybridization, bioisosterism, scaffold hopping, multicomponent reactions, and catalyst-free synthesis) for integrating different functional groups with the pyrazole ring are discussed. Additionally, structure-activity relationships of these pyrazole derivatives, i.e., how structural modifications impact their selectivity and therapeutic potential against bacterial and fungal strains, are highlighted. This review provides insights into designing next-generation antimicrobials to combat AMR, and offers valuable perspectives to the scientists working on heterocyclic compounds with diverse bioactivities.

Antibacterial and Antifungal Pyrazoles Based on Different Construction Strategies

This study demonstrates a strategy involving photoinduced energy transfer for decarboxylative Minisci C–H (amino)alkylation of heteroarenes employing diverse oxime esters (from carboxylic acids) as (amino)alkylating reagents. 

Energy-transfer photocatalysis for Minisci C–H (amino)alkylation of heteroarenes using oxime esters as dual-role reagents

Long-term high altitudes (HA) exposure's impact on cognition has yielded inconsistent findings in previous research. To address this, we conducted a meta-analysis of 49 studies (6,191 individuals) to comprehensively evaluate this effect. Moderating factors such as cognitive task type, altitude (1,500-2,500m, 2,500-4,000m, and above 4,000m), residential type (chronic and lifelong), adaptation level and demographic factors were analyzed. Cognitive tasks were classified into eight categories: perceptual processes, psychomotor function, long-term memory, working memory, inhibitory control, problem-solving, language, and others. Results revealed a moderate negative effect of HA on cognitive performance (g = -.40, SE =.18, 95% CI = -.76 to -.05). Psychomotor function and long-term memory notably experience the most pronounced decline, while working memory and language skills show moderate decreases due to HA exposure. However, perceptual processes, inhibitory control, and problem-solving abilities remain unaffected. Moreover, residing at altitudes above 4,000m and being a HA immigrant are associated with significant cognitive impairment. In summary, our findings indicate a selective adaptation of cognitive performance to HA conditions. 

The effects of long-term high-altitude exposure on cognition: A meta-analysis

Because of the advantages of fluorescent drugs consisting of fluorescent dyes and compounds with anticancer activity for therapeutic diagnostics and personalized medicine. A series of fluorescent antitumor drugs rhodamine pyrimidine derivatives (RP1, RP2, RP3 and RP4) were synthesized by linking rhodamine B and pyrimidine derivatives through ethylenediamine bridge and then introduced into nido-carborane to form fluorescent salt derivatives (RPB1, RPB2, RPB3, and RPB4). It improves the tumor targeting and imaging ability of pyrimidine derivatives. By CCK8, it was found that the inhibition rates of RP4 and RPB4 at 10 μg/mL on HeLa, PC-3 and L02 cells were 70.4 %, 68.7 %, 86.1 % and 72.5 %, 76.4 %, 81.0 %, respectively. The compound has strong inhibitory effect on cancer cells. The logP values of compounds RP4 and RPB4 were between 0 and 3, which were easily absorbed and transported through the cell membrane. Further cell imaging experiments showed that RP4 could enter tumor cells through cell membrane and had good biocompatibility. The experimental results show that compounds RP4 has good imaging capability and tumor targeting, and is a potential fluorescent anticancer agents. 

Design, synthesis, cell imaging, and bioactivity assessment of novel Rhodamine-Pyrimidine nido-carborane derivatives as fluorescent anticancer agents

A visible-light-promoted desulfonylative radical difluoroalkylation between difluoroenol silyl ethers and difluoroalkyl sulfones has been developed.

Visible-light-promoted desulfonylative radical difluoroalkylation between difluoroenol silyl ethers and difluoroalkyl sulfones to construct functionalized aryltetrafluoroethane derivatives

Pyrazole derivatives, as a class of heterocyclic compounds, possess unique chemical structures that confer them with a broad spectrum of pharmacological activities. They have been extensively explored for designing potent and selective anticancer agents. In recent years, numerous pyrazole derivatives have been synthesized and evaluated for their anticancer potential against various cancer cell lines. Structure–activity relationship studies have shown that appropriate substitution on different positions of the pyrazole ring can significantly enhance anticancer efficacy and tumor selectivity. It is noteworthy that many pyrazole derivatives have demonstrated multiple mechanisms of anticancer action by interacting with various targets including tubulin, EGFR, CDK, BTK, and DNA. Therefore, this review summarizes the current understanding on the structural features of pyrazole derivatives and their structure-activity relationships with different targets, aiming to facilitate the development of potential pyrazole-based anticancer drugs. We focus on the latest research advances in anticancer activities of pyrazole compounds reported from 2018 to present.

Recent Advances in the Development of Pyrazole Derivatives as Anticancer Agents

The composite phenotype analysis identifies potential concerted responses of physiological systems to high altitude exposure Yi Li 1,3,9,†, Meng Hao2,4,†, Zixin Hu2,10,†, Yanyun Ma2,3,†, Kun Wang2, Xiaoyu Liu1, Xianhong Yin1, Menghan Zhang 2, Yi Wang2, Meng Liang2, Yuan Guo2, Lei Bao2, Shixuan Zhang2, Shiguan Le1, Chenyuan Wu1, Dayan Sun1, Yang Wei1, Fei Wu2, Rui Zhang1,3, Lingxian Zhu2, Hui Zhang2, Shuai Jiang2,11, Xingdong Chen1,6, Xiaofeng Wang1, Yao Zhang7, Longli Kang7, Wenyuan Duan5, Bin Qiao5, Jiucun Wang1,3,8,∗ and Li Jin1,3,8,9,∗

/pdf/the-composite-phenotype-analysis-identifies-potential-m13wneo8.pdf

The composite phenotype analysis identifies potential concerted responses of physiological systems to high altitude exposure

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Recent Advances in the Development of Pyrazole Derivatives as Anticancer Agents

The composite phenotype analysis identifies potential concerted responses of physiological systems to high altitude exposure