Month: October 2022

Laviron, Etienne published the artcile< Polarographic and physicochemical study of pyridine derivatives and heterocyclic bases. III. Nitro, carbonyl, and halogen-containing derivatives of imidazole>, Quality Control of 1003-21-0, the main research area is .

Exptl. data from polarographic ultraviolet and spectrophotometric measurements showed that the 4 (or 5)-NO2 (or Br) derivative of imidazole exists almost totally as I (R =NO2 or Br) in solution

Bulletin de la Societe Chimique de France published new progress about Ionization. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Quality Control of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Okazaki, Shogo; Noguchi-Yachide, Tomomi; Sakai, Taki; Ishikawa, Minoru; Makishima, Makoto; Hashimoto, Yuichi; Yamaguchi, Takao published the artcile< Discovery of N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel acetyl-CoA carboxylase 2 (ACC2) inhibitors with peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonistic activity>, Reference of 401567-00-8, the main research area is phenoxyphenyloxadiazolylethylacetamide acetyl CoA carboxylase ACC2 inhibitor PPAR agonist; Acetyl-CoA carboxylase; Multi-target drug; Peroxisome proliferator-activated receptor.

Acetyl-Co-A carboxylases (ACCs) catalyze a critical step in de novo lipogenesis, and are considered as promising targets for treatment of obesity, dyslipidemia and type 2 diabetes mellitus. On the other hand, peroxisome proliferator-activated receptors (PPARs) are well-established therapeutic targets for these metabolic syndrome-related diseases. Therefore, the authors considered that dual modulators of ACC and PPARs would be promising candidates as therapeutic agents. Here, the authors designed a series of acetamides based on the mol. similarity between ACC inhibitors and PPAR agonists. Screening of the synthesized compounds identified N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel ACC2 inhibitors with PPARα/PPARδ dual agonistic activity. Structure-activity relationship studies and further structural elaboration afforded compounds with distinct activity profiles. The findings should be helpful for the discovery of candidate agents with an appropriate balance of ACC-inhibitory and PPAR-activating activities for therapeutic lipid control.

Bioorganic & Medicinal Chemistry published new progress about Homo sapiens. 401567-00-8 belongs to class imidazoles-derivatives, and the molecular formula is C8H4ClN3, Reference of 401567-00-8.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Huang, Limin; Hu, Chaoquan; Chao, Hui; Zhang, Yu; Li, Yong; Hou, Jing; Xu, Zhong; Lu, He; Li, Hong; Chen, Hui published the artcile< Drug-resistant endothelial cells facilitate progression, EMT and chemoresistance in nasopharyngeal carcinoma via exosomes>, Category: imidazoles-derivatives, the main research area is nasopharyngeal carcinoma endothelial cell EMT chemoresistance exosome; Drug resistance; Exosome; Human microvascular endothelial cells (HMECs); Nasopharyngeal carcinoma.

Recent antitumor drug development has included investigation of a wide variety of anti-angiogenesis therapies. Because cancer cells in tumors require new blood vessels to grow and spread, they stimulate capillary proliferation from existing vessels as well as new vessel formation from endothelial precursor cells. Our previous findings suggested that drug resistance in mouse endothelial cells supported tumor growth, but the relationship between endothelial cells (ECs) and nasopharyngeal carcinoma (NPC) cells remained unclear. Exosomes are small membrane vesicles that are released by several cell types, including human microvascular ECs (HMECs). Exosomes carrying membrane and cytoplasmic constituents have been described as participants in a novel mechanism of cell-to-cell communication. In the present study, we investigated the mechanisms underlying the interactions between HMECs and NPC cells. We found that drug-resistant HMECs secreted small heterogeneous 40-100 nm vesicles, defined as exosomes. Co-incubation of NPC cells with doxorubicin-resistant (R-DOX) HMEC-derived exosomes resulted in promotion of their proliferation, migration, and chemoresistance, as well as changes in the expression of epithelial-mesenchymal transition (EMT) markers. These effects were significantly inhibited by treatment with GW4869 (an exosome inhibitor). We also found that GW4869 inhibited the stimulation of drug-resistant HMECs on NPC progression by modulating EMT in vivo. These data suggest that exosomes participate in a novel mechanism by which drug-resistant ECs enhance NPC progression.

Cellular Signalling published new progress about Apoptosis. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Category: imidazoles-derivatives.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Liu, Chu-Xiao; Guo, Si-Kun; Nan, Fang; Xu, Yi-Feng; Yang, Li; Chen, Ling-Ling published the artcile< RNA circles with minimized immunogenicity as potent PKR inhibitors>, SDS of cas: 452-06-2, the main research area is RNA immunogenicity PKR inhibitor; PKR; PKR inhibitor; T4 RNA ligase; circular RNA; circular RNA structure; dsRNA; group I intron; immune response; permuted Anabaena pre-tRNA group I intron; phage T4 thymidylate synthase gene.

Exon back-splicing-generated circular RNAs, as a group, can suppress double-stranded RNA (dsRNA)-activated protein kinase R (PKR) in cells. We have sought to synthesize immunogenicity-free, short dsRNA-containing RNA circles as PKR inhibitors. Here, we report that RNA circles synthesized by permuted self-splicing thymidylate synthase (td) introns from T4 bacteriophage or by Anabaena pre-tRNA group I intron could induce an immune response. Autocatalytic splicing introduces ∼74 nt td or ∼186 nt Anabaena extraneous fragments that can distort the folding status of original circular RNAs or form structures themselves to provoke innate immune responses. In contrast, synthesized RNA circles produced by T4 RNA ligase without extraneous fragments exhibit minimized immunogenicity. Importantly, directly ligated circular RNAs that form short dsRNA regions efficiently suppress PKR activation 103- to 106-fold higher than reported chem. compounds C16 and 2-AP, highlighting the future use of circular RNAs as potent inhibitors for diseases related to PKR overreaction.

Molecular Cell published new progress about Anabaena. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, SDS of cas: 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Mardaneh, Jalal; Beyzaei, Hamid; Hashemi, Seyed Hadi; Ghasemi, Behzad; Rahdar, Abbas published the artcile< Comparative evaluation of the inhibitory potential of synthetic N-heterocycles, Cu/Fe3O4@SiO2 nanocomposites and some natural products against non-resistant and antibiotic-resistant Acinetobacter baumannii>, Application In Synthesis of 30086-64-7, the main research area is Acinetobacter Trachyspermum thiazole iron oxide silicon dioxide nanocomposite antibacterial.

Acinetobacter baumannii is a common infectious agent in hospitals. New antimicrobial agents are identified and prepared to combat these bacterial pathogens. In this context, the blocking potentials of a series of synthesized N-heterocyclic compounds, Cu/Fe3O4@SiO2 nanocomposites, glycine, poly-L-lysine, nisin and hydroalcoholic extracts of Trachyspermum ammi, Curcuma longa and green tea catechins were evaluated against non-resistant and multidrug-resistant strains of A. baumannii. Solutions of heterocyclic derivatives and hydroalcoholic extracts of Trachyspermum ammi, Curcuma longa and green tea catechins were prepared at initial concentration of 10240μg ml-1 in 10% DMSO. Other compounds were dissolved in water at the same concentrations Their in vitro inhibitory activity was assessed by determination of IZD, MIC and MBC values. Glycine, poly-L-lysine, nisin, Curcuma longa and green tea catechins extracts, and thiazoles 3a, 3d and 3f were ineffective at their initial concentrations Heterocyclic derivatives 7a-f, 3c, 3e and 3h, Cu/Fe3O4@SiO2 nanocomposites and Trachyspermum ammi extract could block the growth of bacterial strains with IZDs (7.40-15.51 mm), MICs (32-1024μg ml-1) and MBCs (128-2048μg ml-1). Among synthetic chems. and natural products, the best antimicrobial effects were recorded with (E)-2-(5-acetyl-4-methylthiazol-2-yl)-2-(thiazolidin-2-ylidene)acetonitrile (7b) and the extract of Trachyspermum ammi. It is imperative that their toxic and histopathol. effects were assessed in future researches. It is predicted that the essential oil of Trachyspermum ammi will improve its antibacterial activities.

Pharmaceutical Sciences (Tabriz, Islamic Republic of Iran) published new progress about Acinetobacter baumannii. 30086-64-7 belongs to class imidazoles-derivatives, and the molecular formula is C7H12N2S, Application In Synthesis of 30086-64-7.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Li, Jianhua; Liu, Kuancheng; Liu, Yang; Xu, Yan; Zhang, Fei; Yang, Huijuan; Liu, Jiangxia; Pan, Tingting; Chen, Jieliang; Wu, Min; Zhou, Xiaohui; Yuan, Zhenghong published the artcile< Exosomes mediate the cell-to-cell transmission of IFN-α-induced antiviral activity>, Application of C30H30Cl2N6O2, the main research area is IFN alpha induced antiviral activity exosome cell transmission.

The cell-to-cell transmission of viral resistance is a potential mechanism for amplifying the interferon-induced antiviral response. In this study, we report that interferon-α (IFN-α) induced the transfer of resistance to hepatitis B virus (HBV) from nonpermissive liver nonparenchymal cells (LNPCs) to permissive hepatocytes via exosomes. Exosomes from IFN-α-treated LNPCs were rich in mols. with antiviral activity. Moreover, exosomes from LNPCs were internalized by hepatocytes, which mediated the intercellular transfer of antiviral mols. Finally, we found that exosomes also contributed to the antiviral response of IFN-α to mouse hepatitis virus A59 and adenovirus in mice. Thus, we propose an antiviral mechanism of IFN-α activity that involves the induction and intercellular transfer of antiviral mols. via exosomes.

Nature Immunology published new progress about Adenoviridae. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Application of C30H30Cl2N6O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

El Borai, M.; Moustafa, A. H.; Anwar, M.; Ghattas, A. G. published the artcile< Synthesis of new formyl halo N-methylimidazole derivatives>, Category: imidazoles-derivatives, the main research area is imidazole formylbromomethyl; methylimidazole formylation bromination.

Title compounds [I, R, R1, R2 = CHO, Br, H (II), Br, CHO, H; H, Br, CHO; CHO, H, Br; CHO, Br, Br] were prepared E. g., formylation of I (R = Br, R1 = R2 = H) followed by bromination gave II.

Croatica Chemica Acta published new progress about 1003-21-0. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Category: imidazoles-derivatives.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Ishikawa, Ryo; Yasuda, Mizuho; Sasaki, Shogo; Ma, Yue; Nagasawa, Kazuo; Tera, Masayuki published the artcile< Stabilization of telomeric G-quadruplex by ligand binding increases susceptibility to S1 nuclease>, Synthetic Route of 452-06-2, the main research area is stabilization G quadruplex S1 nuclease ligand binding.

The extent of thermodn. stabilization of telomeric G-quadruplex (G4) by isomers of G4 ligand L2H2-6OTD, a telomestatin analog, is inversely correlated with susceptibility to S1 nuclease. L2H2-6OTD facilitated the S1 nuclease activities through the base flipping in G4, unlike the conventional role of G4 ligands which inhibit the protein binding to DNA/RNA upon ligand interactions.

Chemical Communications (Cambridge, United Kingdom) published new progress about Enzyme functional sites, ligand-binding. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Synthetic Route of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem