Month: October 2022

Iddon, Brian; Lim, Bee Lan published the artcile< Metal-halogen exchange reactions of mono- and polyhaloimidazoles>, Application In Synthesis of 1003-21-0, the main research area is exchange lithium halogen haloimidazole; haloimidazole lithiation alkylation; imidazole halo lithiation alkylation; ethoxymethylation lithiation haloimidazole; sulfuration lithiation haloimidazole; alkylhaloimidazole; methylthiophenylthioimidazole; phenylthioimidazole.

Treatment of 4(5)-bromoimidazole with 1-2 equiv BuLi in Et2O or THF followed by reaction with Me2SO4 gave 46-63% of a 1:1-3 mixture of 4- and 5-bromo-1-methylimidazole, resp. 5-Iodo- and 2,4,5-tribromo-1-methylimidazole were similarly prepared N-1-alkylation of tribromoimidazole with ClCH2OEt in C6H6 containing Et3N gave 2,4,5-tribromo-1-(ethoxymethyl)imidazole (I). Similar reaction of 2,4,5-triiodoimidazole required NaOMe in dioxane and gave mainly 1-ethoxymethyl-4,5-diiodoimidazole. Treatment of I with BuLi followed by (PhS)2 gave 67% 4,5-dibromo-1-(ethoxymethyl)-2-phenylthioimidazole, which on further treatment with BuLi followed by (MeS)2 gave 63% 4-bromo-1-(ethoxymethyl)-5-methylthio-2-phenylthioimidazole.

Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) published new progress about Alkylation. 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

Ma, Wenqiang; Xu, Shuangping; Jia, Hongge; Xu, Jingyu; Liu, Da; Zhang, Mingyu; Qu, Yanqing; Zhou, Hailiang; Zhang, Yushu; Wang, Xintian; Zhao, Wenwen published the artcile< Preparation of Butadiene-Bridged Polymethylsiloxane/Ethylcellulose/1-Carboxymethyl-3-methylimidazolium Chloride Ternary Composite Membranes for Gas Separation>, Related Products of 700370-07-6, the main research area is butadiene bridged polymethylsiloxane ethylcellulose composite membrane.

Excessive CO2 emissions have resulted in global warming and are a serious threat to the life of people, various strategies have been implemented to cut carbon emissions, and one of them is the use of a gas separation membrane to capture CO2 effectively. In this experiment, the butadiene-bridged polymethylsiloxane (BBPMS)/ethyl cellulose (EC)/ionic liquid (IL) ternary composite membranes were prepared by EC as a substrate, BBPMS, and IL as additives in THF under high-speed stirring and coated on the membrane. The membrane structure was characterized by a Fourier transform IR spectrometer and scanning electron microscope, and the membrane properties were tested by a membrane tensile strength tester, thermal weight loss analyzer, and gas permeability meter. The results show that the surface of the ternary composite membrane is dense and flat with a uniform distribution, and the membrane formation, heat resistance, and mech. properties are good. The permeability coefficient of the ternary composite membrane for CO2 reached 1806.03 Barrer, which is 20.00 times higher than that of the EC/IL hybrid matrix membrane. The permeability coefficient of O2 reached 321.01 Barrer, which is 19.21 times higher than that of the EC/IL membrane. When the doping amount of BBPMS is 70-80%, the O2/N2 gas permeation separation of the BBPMS/EC/IL ternary composite membrane is close to the Robertson 2008 curve. It is always known that in the gas separation process the membrane material is the most crucial factor. The success of this experiment points to a new direction for the preparation of new membrane materials.

ACS Omega published new progress about Air pollution, carbon dioxide. 700370-07-6 belongs to class imidazoles-derivatives, and the molecular formula is C6H9ClN2O2, Related Products of 700370-07-6.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Szabla, Rafał; Zdrowowicz, Magdalena; Spisz, Paulina; Green, Nicholas J; Stadlbauer, Petr; Kruse, Holger; Šponer, Jiří; Rak, Janusz published the artcile< 2,6-diaminopurine promotes repair of DNA lesions under prebiotic conditions.>, Electric Literature of 452-06-2, the main research area is .

High-yielding and selective prebiotic syntheses of RNA and DNA nucleotides involve UV irradiation to promote the key reaction steps and eradicate biologically irrelevant isomers. While these syntheses were likely enabled by UV-rich prebiotic environment, UV-induced formation of photodamages in polymeric nucleic acids, such as cyclobutane pyrimidine dimers (CPDs), remains the key unresolved issue for the origins of RNA and DNA on Earth. Here, we demonstrate that substitution of adenine with 2,6-diaminopurine enables repair of CPDs with yields reaching 92%. This substantial self-repairing activity originates from excellent electron donating properties of 2,6-diaminopurine in nucleic acid strands. We also show that the deoxyribonucleosides of 2,6-diaminopurine and adenine can be formed under the same prebiotic conditions. Considering that 2,6-diaminopurine was previously shown to increase the rate of nonenzymatic RNA replication, this nucleobase could have played critical roles in the formation of functional and photostable RNA/DNA oligomers in UV-rich prebiotic environments.

Nature communications published new progress about 452-06-2. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Electric Literature of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Yue, Kang-Yi; Zhang, Pei-Ran; Zheng, Min-Hua; Cao, Xiu-Li; Cao, Yuan; Zhang, Yi-Zhe; Zhang, Yu-Fei; Wu, Hai-Ning; Lu, Zhi-Hong; Liang, Liang; Jiang, Xiao-Fan; Han, Hua published the artcile< Neurons can upregulate Cav-1 to increase intake of endothelial cells-derived extracellular vesicles that attenuate apoptosis via miR-1290>, Synthetic Route of 6823-69-4, the main research area is caveolin apoptosis exosome microRNA human neuron.

Extracellular vesicles (EVs) including exosomes can serve as mediators of cell-cell communication under physiol. and pathol. conditions. However, cargo mols. carried by EVs to exert their functions, as well as mechanisms for their regulated release and intake, have been poorly understood. In this study, we examined the effects of endothelial cells-derived EVs on neurons suffering from oxygen-glucose deprivation (OGD), which mimics neuronal ischemia-reperfusion injury in human diseases. In a human umbilical endothelial cell (HUVEC)-neuron coculture assay, we found that HUVECs reduced apoptosis of neurons under OGD, and this effect was compromised by GW4869, a blocker of exosome release. Purified EVs could be internalized by neurons and alleviate neuronal apoptosis under OGD. A miRNA, miR-1290, was highly enriched in HUVECs-derived EVs and was responsible for EV-mediated neuronal protection under OGD. Interestingly, we found that OGD enhanced intake of EVs by neurons cultured in-vitro. We examined the expression of several potential receptors for EV intake and found that caveolin-1 (Cav-1) was upregulated in OGD-treated neurons and mice suffering from middle cerebral artery occlusion (MCAO). Knock-down of Cav-1 in neurons reduced EV intake, and canceled EV-mediated neuronal protection under OGD. HUVEC-derived EVs alleviated MCAO-induced neuronal apoptosis in-vivo. These findings suggested that ischemia likely upregulates Cav-1 expression in neurons to increase EV intake, which protects neurons by attenuating apoptosis via miR-1290.

Cell Death & Disease published new progress about Apoptosis. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Synthetic Route of 6823-69-4.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Huang, Yunlong; Li, Yuju; Zhang, Hainan; Zhao, Runze; Jing, Ran; Xu, Yinghua; He, Miao; Peer, Justin; Kim, Yeong C.; Luo, Jiangtao; Tong, Zenghan; Zheng, Jialin published the artcile< Zika virus propagation and release in human fetal astrocytes can be suppressed by neutral sphingomyelinase-2 inhibitor GW4869>, Computed Properties of 6823-69-4, the main research area is Zika virus infection astrocyte GW4869.

Zika virus (ZIKV) is a neurotrophic flavivirus that is capable of infecting humans, leading to brain abnormalities during fetal development. The ZIKV infectivity in neural target cells remains poorly understood. Here, we found that ZIKV specifically infected glial fibrillary acidic protein- and S100B-pos. primary human astrocytes derived from fetal brains. In contrast, neuron-specific Class III β-tubulin (TuJ1)-pos. neurons in the astrocyte cultures and SOX2-pos. neural progenitor cells derived from the fetal brains were less susceptible to ZIKV infection compared with astrocytes. The infected astrocytes released competent viral particles and manifested programmed cell death with a progressive cytopathic effect. Interestingly, ZIKV infection in human fetal astrocytes induced a significant increase of extracellular vesicles (EVs). Treatment with GW4869, a specific inhibitor of neutral sphingomyelinase-2, decreased EV levels, suppressed ZIKV propagation, and reduced the release of infectious virions in astrocytes. Therefore, ZIKV infects primary human fetal astrocytes and the infection can be suppressed by neutral sphingomyelinase-2 inhibitor GW4869. Further investigation into sphingomyelin metabolism and EVs may provide insights to the therapeutic treatment of ZIKV infection.

Cell Discovery published new progress about Antigens Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Chen, Mingjian; Ma, Changbei; Zhao, Han; Yan, Ying published the artcile< Exonuclease III-assisted fluorometric aptasensor for the carcinoembryonic antigen using graphene oxide and 2-aminopurine>, Recommanded Product: 7H-Purin-2-amine, the main research area is carcinoembryonic antigen exonuclease aptasensor graphene oxide aminopurine; Aptamer; Carcinoembryonic antigen; Enzyme; Fluorescence amplification; Fluorescently labelled probe.

A reliable fluorometric assay is described for the determination carcinoembryonic antigen (CEA) using exonuclease III (Exo III) and a 2-aminopurine binding aptamer. In the absence of CEA, dsDNA is degraded by Exo III, and free 2-AP (which has a blue fluorescence with excitation/emission maxima of 310/365 nm) is released. Strong fluorescence is generated after addition of graphene oxide (GO) to the solution However, the 2-AP modified DNA (T2) cannot be degraded in the presence of CEA by Exo III due to the interaction between CEA and aptamer T1. Hence, only weak fluorescence can be detected after addition of GO. In this system, CEA can be quantified in the 0.05 – 2 ng·mL-1 concentration range with a detection limit of 30 pg·mL-1 (at S/N = 3). The method was successfully applied to analyze serum samples for CEA.

Microchimica Acta 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

Zheng, Yangyang; Hong, Kunqiang; Wang, Baowei; Liu, Dingyu; Chen, Tao; Wang, Zhiwen published the artcile< Genetic Diversity for Accelerating Microbial Adaptive Laboratory Evolution>, Application In Synthesis of 452-06-2, the main research area is review accelerating microbial adaptive laboratory genetic diversity; adaptive laboratory evolution; genetic diversity; genome editing; mutant library.

A review. Adaptive laboratory evolution (ALE) is a widely used and highly effective tool for improving microbial phenotypes and investigating the evolutionary roots of biol. phenomena. Serving as the raw materials of evolution, mutations have been extensively utilized to increase the chances of engineering mols. or microbes with tailor-made functions. The generation of genetic diversity is therefore a core technol. for accelerating ALE, and a high-quality mutant library is crucial to its success. Because of its importance, technologies for generating genetic diversity have undergone rapid development in recent years. Here, we review the existing techniques for the construction of mutant libraries, briefly introduce their mechanisms and applications, discuss ongoing and emerging efforts to apply engineering technologies in the construction of mutant libraries, and suggest future perspectives for library construction.

ACS Synthetic Biology published new progress about Alkylating agents. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Application In Synthesis of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Chen, Jinghua; Xu, Ruilian; Xia, Junxian; Huang, Jiacheng; Su, Binbin; Wang, Senming published the artcile< Aspirin inhibits hypoxia-mediated lung cancer cell stemness and exosome function>, COA of Formula: C30H30Cl2N6O2, the main research area is NSCLC aspirin hypoxia exosome HIF1 microRNA210 SOX2 cell proliferation; Aspirin; Exosomes; Hypoxia; Lung cancer; Stemness.

Epidemiol. studies have illustrated that regular aspirin consumption may decrease the risk of non-small cell lung cancer (NSCLC). The present study aims to investigate the mechanism of aspirin-induced inhibition of NSCLC development during hypoxia. A549 cells were pre-treated with the vehicle control or aspirin and then subjected to hypoxic culture. Cell viability was monitored by CCK-8 assay, and flow cytometry was performed to detect cell cycle distributions, apoptosis, and proportion of cancer stem cells (CSCs). Flow cytometric cell sorting was used to sep. CSCs. Quant. reverse transcription-polymerase chain reaction and Western blot were used to detect the mRNA and protein levels of stem cell markers and the related signaling mols. The abundance of prostaglandin E2 was detected by ELISA. Exosomes in the cell culture medium were isolated using ExoQuick, and the number of exosomes was quantified by the EXOCET exosome quantification assay kit. Cell migration and angiogenesis were monitored by transwell migration assay and in vitro angiogenesis experiments Aspirin inhibited cell proliferation and induced G2/M cell cycle arrest in hypoxic A549 cells; it also inhibited hypoxia-enhanced stemness in both A549 and ALDH+ cells. The drug reduced hypoxia-enhanced numbers of exosomes in A549 cells and exerted neg. effects on the hypoxia-mediated up-regulation of exosomal HIF-1α/COX-2 and expression of exosomal miR-135b and miR-210. While hypoxic-induced exosomes can promote the proliferation, migration, and angiogenesis of other A549 cells, aspirin can weaken this promotion by reducing the amount of exosome secreted and changing exosome contents. Aspirin inhibits the hypoxia-induced stemness, hypoxic-mediated exosome release, and malignant paracrine effects of A549 cells.

Pathology, Research and Practice published new progress about Angiogenesis. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, COA of Formula: C30H30Cl2N6O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Kakiuchi, Yoshihiko; Kuroda, Shinji; Kanaya, Nobuhiko; Kumon, Kento; Tsumura, Tomoko; Hashimoto, Masashi; Yagi, Chiaki; Sugimoto, Ryoma; Hamada, Yuki; Kikuchi, Satoru; Nishizaki, Masahiko; Kagawa, Shunsuke; Tazawa, Hiroshi; Urata, Yasuo; Fujiwara, Toshiyoshi published the artcile< Local oncolytic adenovirotherapy produces an abscopal effect via tumor-derived extracellular vesicles>, Product Details of C30H30Cl2N6O2, the main research area is oncolytic adenovirotherapy tumor derived extracellular vesicle abscopal effect; abscopal effect; drug delivery system; exosome; extracellular vesicles; local treatment; oncolytic adenovirus; systemic delivery.

Extracellular vesicles (EVs) play important roles in various intercellular communication processes. The abscopal effect is an interesting phenomenon in cancer treatment, in which immune activation is generally considered a main factor. We previously developed a telomerase-specific oncolytic adenovirus, Telomelysin (OBP-301), and occasionally observed therapeutic effects on distal tumors after local treatment in immunodeficient mice. In this study, we hypothesized that EVs may be involved in the abscopal effect of OBP-301. EVs isolated from the supernatant of HCT116 human colon carcinoma cells treated with OBP-301 were confirmed to contain OBP-301, and they showed cytotoxic activity (apoptosis and autophagy) similar to OBP-301. In bilateral s.c. HCT116 and CT26 tumor models, intratumoral administration of OBP-301 produced potent antitumor effects on tumors that were not directly treated with OBP-301, involving direct mediation by tumor-derived EVs containing OBP-301. This indicates that immune activation is not the main factor in this abscopal effect. Moreover, tumor-derived EVs exhibited high tumor tropism in orthotopic HCT116 rectal tumors, in which adenovirus E1A and adenovirus type 5 proteins were observed in metastatic liver tumors after localized rectal tumor treatment. In conclusion, local treatment with OBP-301 has the potential to produce abscopal effects via tumor-derived EVs.

Molecular Therapy published new progress about Adenovirus E1A proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Product Details of C30H30Cl2N6O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Yoshida, Tomohiro; Akahoshi, Fumihiko; Sakashita, Hiroshi; Sonda, Shuji; Takeuchi, Masahiro; Tanaka, Yoshihito; Nabeno, Mika; Kishida, Hiroyuki; Miyaguchi, Ikuko; Hayashi, Yoshiharu published the artcile< Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group>, Synthetic Route of 401567-00-8, the main research area is antidiabetic DPP4 inhibitor heteroarylpiperazine prolylthiazolidine preparation structure activity.

Hypoglycemic agents with a mechanism of dipeptidyl peptidase IV (DPP-4) inhibition are suitable for once daily oral dosing. It is difficult to strike a balance between inhibitory activity and duration of action in plasma for inhibitors bearing an electrophilic nitrile group. We explored fused bicyclic heteroarylpiperazine substituted at the γ-position of the proline structure in the investigation of L-prolylthiazolidines lacking the electrophilic nitrile. Among them, 2-trifluoroquinolyl compound 8g is the most potent, long-lasting DPP-4 inhibitor (IC50 = 0.37 nmol/L) with high selectivity against other related peptidases. X-ray crystal structure determination of 8g indicates that CH-π interactions generated between the quinolyl ring and the guanidinyl group of Arg358 enhances the DPP-4 inhibitory activity and selectivity.

Bioorganic & Medicinal Chemistry published new progress about Antidiabetic agents. 401567-00-8 belongs to class imidazoles-derivatives, and the molecular formula is C8H4ClN3, Synthetic Route of 401567-00-8.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem