Category: imidazoles-derivatives

Dong, Yuanlin; Liang, Feng; Huang, Lining; Fang, Fang; Yang, Guang; Tanzi, Rudolph E.; Zhang, Yiying; Quan, Qimin; Xie, Zhongcong published the artcile< The anesthetic sevoflurane induces tau trafficking from neurons to microglia>, Recommanded Product: p-Benzenediacrylanilide, 4′,4′′-di-2-imidazolin-2-yl-, dihydrochloride, the main research area is anesthetic sevoflurane tau trafficking neuron microglia.

Accumulation and spread of tau in Alzheimer’s disease and other tauopathies occur in a prion-like manner. However, the mechanisms and downstream consequences of tau trafficking remain largely unknown. We hypothesized that tau traffics from neurons to microglia via extracellular vesicles (EVs), leading to IL-6 generation and cognitive impairment. We assessed mice and neurons treated with anesthetics sevoflurane and desflurane, and applied nanobeam-sensor technol., an ultrasensitive method, to measure tau/p-tau amounts Sevoflurane, but not desflurane, increased tau or p-tau amounts in blood, neuron culture medium, or EVs. Sevoflurane increased p-tau amounts in brain interstitial fluid. Microglia from tau knockout mice took up tau and p-tau when treated with sevoflurane-conditioned neuron culture medium, leading to IL-6 generation. Tau phosphorylation inhibitor lithium and EVs generation inhibitor GW4869 attenuated tau trafficking. GW4869 mitigated sevoflurane-induced cognitive impairment in mice. Thus, tau trafficking could occur from neurons to microglia to generate IL-6, leading to cognitive impairment.

Communications Biology published new progress about Alzheimer disease. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Recommanded Product: p-Benzenediacrylanilide, 4′,4′′-di-2-imidazolin-2-yl-, dihydrochloride.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Jiang, Dongdong; Gong, Fangyi; Ge, Xuhui; Lv, Chengtang; Huang, Chenyu; Feng, Shuang; Zhou, Zheng; Rong, Yuluo; Wang, Jiaxing; Ji, Chengyue; Chen, Jian; Zhao, Wene; Fan, Jin; Liu, Wei; Cai, Weihua published the artcile< Neuron-derived exosomes-transmitted miR-124-3p protect traumatically injured spinal cord by suppressing the activation of neurotoxic microglia and astrocytes>, Formula: C30H30Cl2N6O2, the main research area is miR124 3p exosome neurotoxic microglia astrocyte spinal cord injury; Astrocytes; Exosomes; Microglia; Spinal cord injury; miR-124-3p/MYH9 axis.

Spinal cord injury (SCI) is a catastrophic injury that can cause irreversible motor dysfunction with high disability. Exosomes participate in the transport of miRNAs and play an essential role in intercellular communication via transfer of genetic material. However, the miRNAs in exosomes which derived from neurons, and the underlying mechanisms by which they contribute to SCI remain unknown. Methods: A contusive in vivo SCI model and a series of in vitro experiments were carried out to explore the therapeutic effects of exosomes. Then, a miRNA microarray anal. and rescue experiments were performed to confirm the role of neuron-derived exosomal miRNA in SCI. Western blot, luciferase activity assay, and RNA-ChIP were used to investigate the underlying mechanisms. Results: The results indicated that neuron-derived exosomes promoted functional behavioral recovery by suppressing the activation of M1 microglia and A1 astrocytes in vivo and in vitro. A miRNA array showed miR-124-3p to be the most enriched in neuron-derived exosomes. MYH9 was identified as the target downstream gene of miR-124-3p. A series of experiments were used to confirm the miR-124-3p/MYH9 axis. Finally, it was found that PI3K/AKT/NF-κB signaling cascades may be involved in the modulation of microglia by exosomal miR-124-3p. Conclusion: A combination of miRNAs and neuron-derived exosomes may be a promising, minimally invasive approach for the treatment of SCI.

Journal of Nanobiotechnology published new progress about Allograft inflammatory factor 1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Formula: C30H30Cl2N6O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Ren, Lingyun; Chen, Shanshan; Yao, Dan; Yan, Hong published the artcile< OxLDL-stimulated macrophage exosomes promote proatherogenic vascular smooth muscle cell viability and invasion via delivering miR-186-5p then inactivating SHIP2 mediated PI3K/AKT/mTOR pathway>, SDS of cas: 6823-69-4, the main research area is lipoprotein macrophage exosome microRNA SHIP2 PI3K AKT atherosclerosis; Atherosclerosis; Exosomes; MiR-186–5p/SHIP2/PI3K/AKT/mTOR; OxLDL-stimulated-macrophages; Vascular smooth muscle cells.

The current study aimed to investigate the implication of microRNA (miRNA) profile in the linkage between oxidized low-d.-lipoprotein (oxLDL)-stimulated-macrophages (MΦ) exosomes and vascular smooth muscle cells (VSMCs) during atherosclerosis. VSMCs were treated by oxLDL-stimulated-MΦ with/without GW4869. MiRNA profile in oxLDL-stimulated-MΦ and untreated-MΦ was detected by microarray, then candidate miRNAs were proposed to RT-qPCR and functional validation in VSMCs. MiR-186-5p mimic/inhibitor was transfected into oxLDL-stimulated-MΦ, then its exosomes were used to VSMCs. Subsequently, miR-186-5p, SHIP2 and PI3K/AKT/mTOR pathway were modified alone or in combination in VSMCs. VSMCs viability, invasion and apoptosis were detected. OxLDL-stimulated-MΦ induced VSMCs viability, invasion, but repressed apoptosis (all P < 0.01); while after GW4869 treatment to delete exosomes, its effect was weakened (all P < 0.05). Totally 45 dysregulated miRNAs were identified in oxLDL-stimulated-MΦ vs. untreated-MΦ. The top-three dysregulated miRNAs (miR-186-5p, miR-21-5p, miR-320b) were elevated in VSMCs after oxLDL-stimulated-MΦ treatment (all P < 0.001); while only miR-186-5p mimic greatly enhanced VSMCs viability and invasion (both P < 0.01). Furthermore, miR-186-5p-overexpressed oxLDL-stimulated-MΦ exosomes promoted VSMCs viability, invasion, repressed apoptosis, while miR-186-5p-knockdown oxLDL-stimulated-MΦ exosomes exhibited opposite effect (all P < 0.05). MiR-186-5p neg. regulated SHIP2 in VSMCs and bound SHIP2 via luciferase-reporter-gene assay (all P < 0.05). SHIP2 overexpression decreased VSMCs viability, invasion, PI3K/AKT/mTOR pathway, increased apoptosis, and attenuated miR-186-5p-overexpression's effect on these functions (all P < 0.05). Besides, PI3K activator (740 Y-P) weakened SHIP2-overexpression's effect on VSMCs viability, invasion and apoptosis (all P < 0.05). In conclusion, oxLDL-stimulated-MΦ exosomes deliver miR-186-5p to inactivate SHIP2 mediated PI3K/AKT/mTOR pathway, then promote cell viability and invasion in VSMCs to accelerate atherosclerosis. Molecular Immunology published new progress about Apoptosis. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, SDS of cas: 6823-69-4.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Niu, Ziru; Pang, Ronald T. K.; Liu, Weimin; Li, Qian; Cheng, Ranran; Yeung, William S. B. published the artcile< Polymer-based precipitation preserves biological activities of extracellular vesicles from an endometrial cell line>, Computed Properties of 6823-69-4, the main research area is extracellular vesicle endometrial cell uterine luminal fluid; biol activity polymer based precipitation.

Extracellular vesicles (EVs) are membrane-bound vesicles released by cells and act as media for transfer of proteins, small RNAs and mRNAs to distant sites. They can be isolated by different methods. However, the biol. activities of the purified EVs have seldom been studied. In this study, we compared the use of ultracentrifugation (UC), ultra-filtration (UF), polymer-based precipitation (PBP), and PBP with size-based purification (PBP+SP) for isolation of EVs from human endometrial cells and mouse uterine luminal fluid (ULF). Electron microscopy revealed that the diameters of the isolated EVs were similar among the tested methods. UF recovered the highest number of EVs followed by PBP, while UC and PBP+SP were significantly less efficient (P<0.05). Based on the number of EVs-to-protein ratios, PBP had the least protein contamination, significantly better than the other methods (P<0.05). All the isolated EVs expressed exosome-enriched proteins CD63, TSG101 and HSP70. Incubation of the trophoblast JEG-3 cells with an equal amount of the fluorescence-labeled EVs isolated by the studied methods showed that many of the PBP-EVs treated cells were fluorescence pos. but only a few cells were labeled in the UC- and UF-EVs treated groups. Moreover, the PBP-EVs could transfer significantly more miRNA to the recipient cells than the other 3 methods (P<0.05). The PBP method could isolate EVs from mouse ULF; the diameter of the isolated EVs was 62 ± 19 nm and expressed CD63, TSG101 and HSP70 proteins. In conclusion, PBP could best preserve the activities of the isolated EVs among the 4 methods studied and was able to isolate EVs from a small volume of sample. The simple setup and low equipment demands makes PBP the most suitable method for rapid EV assessment and isolation of EVs in clin. and basic research settings. PLoS One published new progress about Blastocyst. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Computed Properties of 6823-69-4.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Ghosh, Tonmoy; Mondal, Aniruddha; Vamsi Bharadwaj, S. V.; Mishra, Sandhya published the artcile< A naturally fluorescent protein C-phycoerythrin and graphene oxide bio-composite as a selective fluorescence ""turn off/on"" probe for DNA quantification and characterization>, Recommanded Product: 7H-Purin-2-amine, the main research area is C phycoerythrin graphene oxide DNA quantification fluorescence characterization; C-phycoerythrin; DNA sensing; Fluorescence quenching; Graphene oxide; Protein – graphene oxide interaction.

Highly specific graphene-DNA interactions have been at the forefront of graphene-based sensor design for various analytes, including DNA itself. However, in addition to its detection, DNA also needs to be characterized according to its size and concentration in a sample, which is an addnl. anal. step. Designing a highly sensitive and selective DNA sensing and characterization platform is, thus, of great interest. The present study demonstrates that a bio-derived, naturally fluorescent protein C-phycoerythrin (CPE) – graphene oxide (GO) bio-composite can be used to detect dsDNA in nanomolar quantities efficiently via fluorescent “”turn off/on”” mechanism. Interaction with GO temporarily quenches CPE fluorescence in a dose-dependent manner. Anal. characterization indicates an indirect charge transfer with a corresponding loss of crystalline GO structure. The fluorescence is regained with the addition of DNA, while other biomols. do not pose any hinderance in the detection process. The extent of regain is DNA length dependent, and the corresponding calibration curve successfully quantifies the size of an unknown DNA. The incubation time for detection is ∼3-5 min. The bio-composite platform also works successfully in a complex biomol. matrix and cell lysate. However, the presence of serum albumin poses a hinderance in the serum sample. Particle size anal. proves that CPE displacement from GO surface by the incoming DNA is the reason for the “”turn on”” response, and that the sensing process is exclusive to dsDNA. This new platform could be an exciting and rapid DNA sensing and characterization tool.

International Journal of Biological Macromolecules published new progress about Albumins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Recommanded Product: 7H-Purin-2-amine.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

He, Yanhua; Yu, Youwei; Wen, Xiaoye; Shi, Yan; Wu, Jianhu; Guan, Zhengping; Cui, Meilin; Xiao, Chunling published the artcile< A quencher-free 2-aminopurine modified hairpin aptasensor for ultrasensitive detection of Ochratoxin A>, Recommanded Product: 7H-Purin-2-amine, the main research area is aminopurine hairpin aptasensor Ochratoxin A fluorescence quenching; 2-Aminopurine; Aptasensor; Exonuclease I; Ochratoxin A; Quencher-free.

A sensitive, efficient and quencher-free fluorescence aptasensor to detect Ochratoxin A (OTA) based on aptamer, 2-aminopurine (2AP) labeled Oligonucleotide sequence, as well as exonuclease I (Exo I) activity was developed. In which the aptamer specific to OTA was modified into a hairpin structure, and 8 bases at the 3′ ends are exposed (H); also, 2AP is embedded in the oligonucleotide complementary to the 8 bases (2AP-probe). The detection principle based on 2AP-probe could be bonded to its complementary sequence and quenches the fluorescence of 2AP; The aptamer has a stronger affinity for the target than its complementary sequence; Exo I can dissociate single-stranded DNA and has little effect on double-stranded DNA as well as folded DNA. In the absence of OTA, the fluorescence of 2AP is quenched due to the complementary pairing of H and 2AP-probe; in the presence of OTA, H selective binding target is detached from 2AP-probe, and the fluorescence of 2AP is slightly restored. Moreover, when the Exo I is added to the detection system, 2AP-probe is dissociated by the Exo I to release the free 2AP, and the fluorescence of the system is further enhanced thereby realizing the detection of OTA. The detection limit of the aptasensor was low as 0.03 nM with a linear range of 0.5-100 nM. Moreover, the aptasensor has good selectivity and practicability and also has good potential in realizing the detection of toxic and harmful substances in food complex matrixes.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about Aptasensors. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Recommanded Product: 7H-Purin-2-amine.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Kauffmann, Thomas; Nuernberg, Reinhard; Schulz, Jutta; Stabba, R. published the artcile< Hetarynes. X. Detection of a 5-membered ring aryne (1-methyl-4,5-dehydroimidazole)>, Application In Synthesis of 1003-21-0, the main research area is IMIDAZOLES ARYNE; DEHYDROIMIDAZOLES; ARYNE IMIDAZOLES.

Treating 5-chloro-1-methylimidazole (I) and 5-bromol-1-methylimidazole (II) with Li piperidide/piperidine (III) in boiling ether gave a mixture of 4-piperidino-1-methylimidazole (IV) and 5-piperidino-1-methylimidazole (V). Analogous results using Li pyrrolidide (VI)/pyrrolidine (VII) base pair suggested that IV and V were formed through an elimination-addition mechanism on the title compound (VIII). The mechanism was elucidated by competing reactions of I and II with varying ratios of VII-III base pairs which resulted in IV, V, 5-pyrrolidinyl-1-methylimidazole, and 4-pyrrolidinyl-1-methylimidazole (IX). Anal. of product distribution indicated that the rearranged substitution products IV and IX were prepared through the elimination-addition mechanism, whereas the non-rearranged substitution products resulted from an overlap of the elimination-addition and the normal addition-elimination mechanism, in each case confirming the presence of VIII. Study on competitive reaction of 3-chloropyridine and 4-chloropyridine with the base-pair diethylamine/diisopropylamine confirmed the conclusion that all reactions with II follow the elimination-addition mechanism over the poorly selective intermediate VIII. With chloro compounds such as I, the normal addition-elimination mechanism becomes more important.

Tetrahedron Letters published new progress about 1003-21-0. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Application In Synthesis of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Li, Peng; Herrmann, Wolfgang A.; Kuehn, Fritz E. published the artcile< Unsaturated NHC Complexes Immobilized by the Backbone: Synthesis and Application>, Application In Synthesis of 1003-21-0, the main research area is silica rhodium heterocyclic carbene complex catalyst styrene hydrogenation ethylbenzene.

The synthesis and an exemplary catalytic application of a SBA-15-supported rhodium-N-heterocyclic carbene (NHC) complex is reported. In contrast to the conventional method of immobilization of unsaturated NHC complexes, the rhodium-NHC compound described here is connected to the SBA-15 surface by a linker originating from the backbone of the unsaturated NHC ligand. The unique characteristics of the new immobilization mode enable the supported NHC complexes to maintain two unchanged “”wing-tip”” ligands. This method of immobilization of unsaturated NHC complexes provides a new way to maintain the original configuration of homogeneous NHC complexes in the heterogenized catalytic system. The immobilized rhodium-NHC catalyst is used in a hydrogenation reaction with styrene as substrate.

ChemCatChem published new progress about Catalyst supports. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Application In Synthesis of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Xu, Guozhang; Liu, Zhijie; Wang, Xinkang; Lu, Tianbao; DesJarlais, Renee L.; Thieu, Tho; Zhang, Jing; Devine, Zheng Huang; Du, Fuyong; Li, Qiu; Milligan, Cynthia M.; Shaffer, Paul; Cedervall, Peder E.; Spurlino, John C.; Stratton, Christopher F.; Pietrak, Beth; Szewczuk, Lawrence M.; Wong, Victoria; Steele, Ruth A.; Bruinzeel, Wouter; Chintala, Madhu; Silva, Jose; Gaul, Michael D.; Macielag, Mark J.; Nargund, Ravi published the artcile< Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions>, Formula: C4H5BrN2, the main research area is cyclopropylpyrazolyl pyridine oxide preparation anticoagulation docking SAR.

Herein, activated factor XI (FXIa) inhibitors novel anticoagulants, discovery effort, utilizing nonclassical interactions to improve potency, cellular permeability, and oral bioavailability by enhancing the binding while reducing polar atoms was described. Beginning with literature-inspired pyridine N-oxide-based FXIa inhibitor 1, the imidazole linker was first replaced with a pyrazole moiety to establish a polar C-H···water hydrogen-bonding interaction. Then, structure-based drug design was employed to modify lead mol. I in the P1′ and P2′ regions, with substituents interacting with key residues through various nonclassical interactions. As a result, a potent FXIa inhibitor II (Ki = 0.17 nM) was discovered. This compound demonstrated oral bioavailability in preclin. species (rat 36.4%, dog 80.5%, and monkey 43.0%) and displayed a dose-dependent antithrombotic effect in a rabbit arteriovenous shunt model of thrombosis.

Journal of Medicinal Chemistry published new progress about Anticoagulants, oral. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Formula: C4H5BrN2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Yang, Zhouping; Liu, Yaqing; Liu, Yang; Wang, Yanying; Rao, Hanbing; Liu, Yong; Yin, Jiajian; Yue, Guizhou; Wu, Caimei; Li, Hua; Liu, Xiaopeng; Wang, Xianxiang published the artcile< Preparation of porous uranium oxide hollow nanospheres with peroxidase mimicking activity: application to the colorimetric determination of tin(II)>, Product Details of C6H9ClN2O2, the main research area is uranium oxide nanosphere peroxidase ionic liquid tin colorimetry detection; Ionic liquids; Nuclear materials; Peroxidase mimic; Uranium oxide.

Porous uranium oxide hollow sphere nanoparticles were synthesized in ionic liquids under hydrothermal conditions. Various precipitating agents and ionic liquids were investigated to determine their resp. impact on the resultant uranium oxide morphologies. Using hydrazine hydrate as precipitating agent and N-Bu pyridinium bromide as templating agent, a porous-hollow structure was created with a surface area of 1958 m2.g-1 and an average pore diameter of 30 nm. The nanoparticles revealed high peroxidase-mimicking activity. This was evaluated by using the peroxidase substrate 3,3′,5,5′-tetramethylbenzidine (TMB) that is catalytically oxidized by H2O2 to give oxidized TMB (oxTMB) which is blue (with an absorption peak at 652 nm). The material was used as a nanozyme for colorimetric detection of Sn2+. Meanwhile, it is found that BSA strongly improves the catalytic activity of the nanozyme, while Sn(II) inhibits its activity. Thus, a colorimetric method for Sn2+ detection was designed. The method works in the 0.5-100μM Sn(II) concentration range and has a lower detection limit of 0.36μM (at S/N = 3).

Microchimica Acta published new progress about Binding energy. 700370-07-6 belongs to class imidazoles-derivatives, and the molecular formula is C6H9ClN2O2, Product Details of C6H9ClN2O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem