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6-Bromoindole- and 6-Bromoindazole-Based Inhibitors of Bacterial Cystathionine γ-Lyase Containing 3-Aminothiophene-2-Carboxylate Moiety.
Molecules
January 2025
Engelhardt Institute of Molecular Biology of the Russian Academy of Sciences, 32 Vavilov St., Moscow 119991, Russia.
In recent years, a number of synthetic potentiators of antibiotics have been discovered. Their action can significantly enhance the antibacterial effect and limit the spread of antibiotic resistance through inhibition of bacterial cystathionine-γ-lyase. To expand the known set of potentiators, we developed methods for the synthesis of five new representatives of 6-bromoindole derivatives-potential inhibitors of bacterial cystathionine-γ-lyase-namely potassium 3-amino-5-((6-bromoindolyl)methyl)thiophene-2-carboxylate () and its 6-bromoindazole analogs ( and ), along with two 6-broindazole analogs of the parent compound .
View Article and Find Full Text PDFRapid access to functionalized nanographenes through a palladium-catalyzed multi-annulation sequence.
Chem Sci
January 2025
Institute of Chemistry, Academia Sinica 128 Academia Road, Section 2, Nankang Taipei 115201 Taiwan
Nanographenes and polycyclic aromatic hydrocarbons exhibit many intriguing physical properties and have potential applications across a range of scientific fields, including electronics, catalysis, and biomedicine. To accelerate the development of such applications, efficient and reliable methods for accessing functionalized analogs are required. Herein, we report the efficient synthesis of functionalized small nanographenes from readily available iodobiaryl and diarylacetylene derivatives a one-pot, multi-annulation sequence catalyzed by a single palladium catalyst.
View Article and Find Full Text PDFMonitoring CO as a plant signaling molecule under heavy metal stress using carbon nanodots.
Dalton Trans
January 2025
Department of Chemistry, Visva-Bharati University, Santiniketan-731235, India.
Carbon monoxide (CO) is widely recognized as a significant environmental pollutant and is associated with numerous instances of accidental poisoning in humans. However, it also serves a pivotal role as a signaling molecule in plants, exhibiting functions analogous to those of other gaseous signaling molecules, including nitric oxide (NO) and hydrogen sulfide (HS). In plant physiology, CO is synthesized as an integral component of the defense mechanism against oxidative damage, particularly under abiotic stress conditions such as drought, salinity, and exposure to heavy metals.
View Article and Find Full Text PDFDesign, synthesis, in-vitro and in-silico studies of novel N-heterocycle based hydrazones as α-glucosidase inhibitors.
Bioorg Chem
January 2025
Department of Pharmacy, University of Genoa, Viale Benedetto XV, 3, Genoa 16132, Italy. Electronic address:
Diabetes mellitus has dominated the globe as a chronic health condition and has become a major global health concern. The inhibition of the key metabolic enzymes of carbohydrates digestion including α-amylase and α-glucosidase are the promising targets for the treatment of diabetes via delaying glucose absorption. Therefore, nitrogen containing saturated heterocycle (pyrrolidinyl, piperidinyl and N-methylpiperazinyl) based hydrazones derivatives 5-23 were synthesized through two step reactions and evaluated for their anti-diabetic potential.
View Article and Find Full Text PDFClinical efficacy of dexmedetomidine preemptive analgesia in breast tumor resection.
Am J Transl Res
December 2024
Department of Anesthesiology, Tianjin Medical University Cancer Institute and Hospital Tianjin 300060, China.
Objective: To investigate the clinical efficacy of dexmedetomidine preemptive analgesia in patients undergoing mastectomy.
Methods: A retrospective study was conducted, including 236 patients who underwent breast tumor resection. Of these, 131 patients in the control group received routine postoperative intravenous patient-controlled analgesia, while 105 patients in the preemptive analgesia group received dexmedetomidine preemptive analgesia during surgery.
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