Day: October 18, 2022

Lu, Cuifen; Nie, Junqi; Yang, Guichun; Chen, Zuxing published the artcile< An improved synthesis of sitophilure>, Category: thiazole, the main research area is asym synthesis sitophilure aldol reaction chiral auxiliary.

The asym. synthesis of sitophilure (I) was carried out in 8 steps, with 42% overall yield and 97% enantiomeric excess from propionaldehyde. The synthesis relied on an approach employing an asym. acyl-thiazolidinethione propionate aldol reaction to establish two stereogenic centers.

Canadian Journal of Chemistry published new progress about Aldol condensation, stereoselective. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Category: thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Vagadia, F. J.; Bhuva, D. A.; Jiladia, M. A. published the artcile< Synthesis and antimicrobial evaluation of some novel substituted thiazole derivatives>, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is thiazole azetidinone preparation antibacterial antifungal.

2-Aminothiazoles were prepared by condensation reaction of acetophenones and thiourea. Subsequent reaction with aromatic aldehydes gave Schiff bases, which were were cyclized with ClCH2COCl and Et3N to yield 2-azetidinones. The synthesized compounds were screened for antibacterial (E. coli, S. aureus) and antifungal (C. albicans) activity by disk diffusion and showed weak to moderate activity.

Pharma Science Monitor published new progress about Antibacterial agents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Volgraf, Matthew; Sellers, Benjamin D.; Jiang, Yu; Wu, Guosheng; Ly, Cuong Q.; Villemure, Elisia; Pastor, Richard M.; Yuen, Po-wai; Lu, Aijun; Luo, Xifeng; Liu, Mingcui; Zhang, Shun; Sun, Liang; Fu, Yuhong; Lupardus, Patrick J.; Wallweber, Heidi J. A.; Liederer, Bianca M.; Deshmukh, Gauri; Plise, Emile; Tay, Suzanne; Reynen, Paul; Herrington, James; Gustafson, Amy; Liu, Yichin; Dirksen, Akim; Dietz, Matthias G. A.; Liu, Yanzhou; Wang, Tzu-Ming; Hanson, Jesse E.; Hackos, David; Scearce-Levie, Kimberly; Schwarz, Jacob B. published the artcile< Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design>, Formula: C7H10N2O2S, the main research area is NMDA receptor allosteric modulator PAM deactivation structure design; crystal structure.

The N-methyl-D-aspartate receptor (NMDAR) is a Na+ and Ca2+ permeable ionotropic glutamate receptor that is activated by the coagonists glycine and glutamate. NMDARs are critical to synaptic signaling and plasticity, and their dysfunction has been implicated in a number of neurol. disorders, including schizophrenia, depression, and Alzheimer’s disease. Herein we describe the discovery of potent GluN2A-selective NMDAR pos. allosteric modulators (PAMs) starting from a high-throughput screening hit. Using structure-based design, we sought to increase potency at the GluN2A subtype, while improving selectivity against related α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs). The structure-activity relationship of channel deactivation kinetics was studied using a combination of electrophysiol. and protein crystallog. Effective incorporation of these strategies resulted in the discovery of GNE-0723 (46), a highly potent and brain penetrant GluN2A-selective NMDAR PAM suitable for in vivo characterization.

Journal of Medicinal Chemistry published new progress about Crystal structure. 72054-60-5 belongs to class thiazole, and the molecular formula is C7H10N2O2S, Formula: C7H10N2O2S.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Inouye, Satoshi; Nakamura, Mitsuhiro; Taguchi, Jumpei; Hosoya, Takamitsu published the artcile< Identification of a novel oxidation product from yellow fluorophore in the complex of apoPholasin and dehydrocoelenterazine>, Application of C11H8N2O3S2, the main research area is oxidation yellow fluorophore complex apoPholasin dehydrocoelenterazine; Coelenteramide; Coelenteramine; Coelenterazine; Photoproteins; Reactive oxygen.

The complex of the recombinant fusion protein of apoPholasin and glutathione S-transferase (GST-apoPholasin) with non-fluorescent dehydrocoelenterazine (dCTZ) (GST-apoPholasin/dCTZ complex) shows yellow fluorescence at 539 nm by excitation at 430 nm. The GST-apoPholasin/dCTZ complex with a fluorophore (dCTZ*) has considerably weak luminescence activity, converting slowly to a blue fluorescence protein with the emission peak at 430 nm. The main oxidation products from dCTZ* for blue fluorescence were identified as coelenteramine (CTM) and an unreported pyrazine derivative, 3-benzyl-5-(4-hydroxyphenyl)pyrazin-2(1H)-one (CTO) that was confirmed by chem. synthesis.

Bioorganic & Medicinal Chemistry Letters published new progress about Chimeric fusion proteins Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (GST-apoPholasin). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application of C11H8N2O3S2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Shergalis, Andrea; Xue, Ding; Gharbia, Fatma Z.; Driks, Hannah; Shrestha, Binita; Tanweer, Amina; Cromer, Kirin; Ljungman, Mats; Neamati, Nouri published the artcile< Characterization of Aminobenzylphenols as Protein Disulfide Isomerase Inhibitors in Glioblastoma Cell Lines>, Synthetic Route of 198904-53-9, the main research area is aminobenzylphenol structure screening preparation PDIA1 inhibitor glioblastoma.

Disulfide bond formation is a critical post-translational modification of newly synthesized polypeptides in the oxidizing environment of the endoplasmic reticulum and is mediated by protein disulfide isomerase (PDIA1). In this study, we report a series of α-aminobenzylphenol analogs as potent PDI inhibitors. The lead compound, AS15, is a covalent nanomolar inhibitor of PDI, and the combination of AS15 analogs with glutathione synthesis inhibitor buthionine sulfoximine (BSO) leads to synergistic cell growth inhibition. Using nascent RNA sequencing, we show that an AS15 analog triggers the unfolded protein response in glioblastoma cells. A BODIPY-labeled analog binds proteins including PDIA1, suggesting that the compounds are cell-permeable and reach the intended target. Taken together, these findings demonstrate an extensive biochem. characterization of a novel series of highly potent reactive small mols. that covalently bind to PDI.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 198904-53-9 belongs to class thiazole, and the molecular formula is C10H7NOS, Synthetic Route of 198904-53-9.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Zhao, Pei; Wu, Xiaokang; Li, Jie; Dong, Gaopan; Sun, Yingai; Ma, Zhao; Li, Minyong; Du, Lupei published the artcile< Discovery of alkene-conjugated luciferins for redshifted and improved bioluminescence imaging in vitro and in vivo>, Formula: C11H8N2O3S2, the main research area is .

The firefly luciferase system is the most extensively utilized bioluminescence system in the field of life science at the moment. In this work, we designed and synthesized a series of alkene-conjugated luciferins to develop new firefly bioluminescence substrates, and further evaluated their activities in vitro and in vivo. It is worth noting that the maximum biol. emission wavelength of novel luciferin analog AL3 ((S,E)-2-(6-hydroxy-5-(3-methoxy-3-oxoprop-1-en-1-yl)benzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid) is 100 nm red-shifted compared with D-luciferin, while that of analog AL4 ((S,E)-2-(5-(2-cyanovinyl)-6-hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid) is 75 nm red-shifted. The new substrate AL2 ((S,E)-2-(6-hydroxy-7-(3-methoxy-3-oxoprop-1-en-1-yl)benzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid) showed better bioluminescence performance in vivo.

Organic & Biomolecular Chemistry published new progress about 2591-17-5. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Formula: C11H8N2O3S2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Yu, Dou; Li, Gina; Lesniak, Maciej S.; Balyasnikova, Irina V. published the artcile< Intranasal delivery of therapeutic stem cells to glioblastoma in a mouse model>, Quality Control of 115144-35-9, the main research area is intranasal administration stem cell therapy glioblastoma.

The intrinsic tropism towards brain malignancies renders stem cells as promising carriers of therapeutic agents against malignant tumors. The delivery of therapeutic stem cells via the intranasal route is a recently discovered alternative strategy, with strong potential for clin. translation, due to its non-invasive nature compared to intracranial implantation or delivery via systemic routes. The lack of blood brain barrier further strengthens the therapeutic potential of stem cells undergoing intranasal brain entry. This article summarizes the essential techniques utilized in our studies and outlines the basic principles of intranasal strategy for stem cell delivery using a mouse model of intracranial glioma xenografts. We demonstrate the optimized procedures that generate consistent and reproducible results with specific predetermined exptl. parameters and offer guidelines for streamlined work flow that ensure efficient execution and reliable exptl. outcome. The article is designed to serve as a baseline for further exptl. customization based on hypothesis, stem cell types, or tumor specifics.

Journal of Visualized Experiments published new progress about Adenoviral vectors. 115144-35-9 belongs to class thiazole, and the molecular formula is C11H7KN2O3S2, Quality Control of 115144-35-9.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Bellini, Michela; Riva, Benedetta; Tinelli, Veronica; Rizzuto, Maria Antonietta; Salvioni, Lucia; Colombo, Miriam; Mingozzi, Francesca; Visioli, Alberto; Marongiu, Laura; Frascotti, Gianni; Christodoulou, Michael S.; Passarella, Daniele; Prosperi, Davide; Fiandra, Luisa published the artcile< Engineered Ferritin Nanoparticles for the Bioluminescence Tracking of Nanodrug Delivery in Cancer>, Synthetic Route of 115144-35-9, the main research area is ferritin nanoparticle bioluminescence imaging cancer; apoferritin nanoparticles; luciferase/luciferin; nanomedicine; self-immolative linkers; tumor targeting.

The identification of a highly sensitive method to check the delivery of administered nanodrugs into the tumor cells is a crucial step of preclin. studies aimed to develop new nanoformulated cures, since it allows the real therapeutic potential of these devices to be forecast. In the present work, the ability of an H-ferritin (HFn) nanocage, already investigated as a powerful tool for cancer therapy thanks to its ability to actively interact with the transferrin receptor 1, to act as an efficient probe for the monitoring of nanodrug delivery to tumors is demonstrated. The final formulation is a bioluminescent nanoparticle, where the luciferin probe is conjugated on nanoparticle surface by means of a disulfide containing linker (Luc-linker@HFn) which is subjected to glutathione-induced cyclization in tumor cell cytoplasm. The prolonged imaging of luciferase+ tumor models, demonstrated by an in vitro and an in vivo approach, associated with the prolonged release of luciferin into cancer cells by disulfide bridge reduction, clearly indicates the high efficiency of Luc-linker@HFn for drug delivery to the tumor tissues.

Small published new progress about Apoferritins Role: NAN (Nanomaterial), THU (Therapeutic Use), BIOL (Biological Study), USES (Uses). 115144-35-9 belongs to class thiazole, and the molecular formula is C11H7KN2O3S2, Synthetic Route of 115144-35-9.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Zhang, Zhi-Hua; Wu, Hong-Mei; Deng, Sai-Nan; Cai, Xiao-Yu; Yao, Yu; Mwenda, Muriira Cyrus; Wang, Jin-Yin; Cai, Dong; Chen, Yu published the artcile< Design, synthesis, and anticancer activities of novel 2-amino-4-phenylthiazole scaffold containing amide moieties>, Quality Control of 57493-24-0, the main research area is morpholinoacetamido thiazolylphenyl benzamide preparation anticancer activity.

Appropriately substituted 2-amino-4-phenylthiazole derivatives I (R = 3-CH3C6H4, 4-BrC6H4, 2-furyl, cyclohexyl, CH3OCH2, ClCH2, etc.) were designed and synthesized according to the structural characteriztics of crizotinib. The target compounds I were evaluated for their in vitro antiproliferative activity against A549, HeLa, HT29, and Karpas299 human cancer cell lines. Based on results of biol. studies, some of these compounds exhibited significant antiproliferative activity. Compound I (R = 3,4-Cl2C6H3) possessed outstanding growth inhibitory effects on the four cell lines, especially for HT29 cell with IC50 value of 2.01 μM. Along with the biol. assay data, a mol. docking study suggests that the target compounds were a potential inhibitor.

Journal of Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Quality Control of 57493-24-0.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Lyashchuk, S. N.; Enya, V. I.; Doroshenko, T. F.; Skrypnik, Yu. G. published the artcile< Study of reaction routes in sulfonation of 2-aminothiazoles with chlorosulfonic acid>, HPLC of Formula: 57493-24-0, the main research area is thiazole amine sulfonation thermal isomerization thiazolesulfonic thiazolesulfamic acid preparation; charge distribution thiazole amine AM1 calculation sulfonation mechanism.

The sulfonation of 4-substituted 2-aminothiazoles with chlorosulfonic acid under mild conditions afforded primarily C-sulfonation product, 2-amino-5-thiazolesulfonic acids, which undergo thermal isomerization by heating in sulfuric acid into the corresponding stable 2-thiazolesulfamic acids. Reaction of 4-R-thiazole-2-amines (9-12) with ClSO3H gave 2-amino-4-R-thiazole-5-sulfonic acids (1-4; R = Me, 4-BrC6H4, 3-O2NC6H4, 4-ClC6H4); heating of 1-4 at 110° in concentrate H2SO4 gave 4-R-thiazole-2-sulfamic acids (5-8). Quantum chem. calculations at AM1 level revealed the presence of considerable neg. charge on the C-5 atom of the thiazole ring of 9-12, which accounts for the opposite sulfonation patterns for the aminothiazoles and aniline.

Russian Journal of Organic Chemistry published new progress about AM1 (molecular orbital method). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, HPLC of Formula: 57493-24-0.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica