Day: December 1, 2022

Praveen, Aletti S. published the artcileSynthesis, characterization and antimicrobial studies of a few novel thiazole derivatives, Quality Control of 64987-16-2, the publication is Medicinal Chemistry Research (2014), 23(1), 259-268, database is CAplus.

A series of novel N-[4-(substituted)-1,3-thiazol-2-yl]-2-(substituted)acetamides and Me 2-(2-(2-(substituted)acetamido)thiazol-4-yl)acetates were synthesized. All compounds were screened for their in vitro antibacterial activity against S. aureus, E. coli, P. aeruginosa, and K. pneumonia by disk diffusion and for antifungal activity against P. marneffei, T. mentagrophytes, A. flavus, and A. fumigatus by serial plate dilution Some of the compounds exhibited growth inhibition against all the tested bacterial strains, with MIC of 12.5-6.25 μg/mL. Among the compounds tested for antifungal activity, several of them showed a wide range of activity against all the tested strains. Most of the newly synthesized compounds were effective against fungal strains rather than bacterial strains. However, some of the compounds showed selective sensitivity against some of the bacterial strains, whereas they were unable to sustain the growth of other strains.

Medicinal Chemistry Research published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Quality Control of 64987-16-2.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Wu, Feng published the artcileSynthesis and evaluation of novel 2,4-diaminopyrimidines bearing a sulfoxide moiety as anaplastic lymphoma kinase (ALK) inhibition agents, Product Details of C7H5ClN2S, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 128253, database is CAplus and MEDLINE.

Herein, 16 new 2,4-diaminopyrimidines I (R¹ = H, F, Cl; R² = EtS, EtSO, i-PrSO; R³ = Me₂NCH₂CH₂NMe, 4-methylpiperazin-1-yl, 4-methyl-1,4-diazepan-1-yl, 4-dimethylaminopiperidin-1-yl, etc.; R⁴ = H, H₂N, EtCONH) bearing a sulfide or sulfoxide moiety were synthesized and evaluated for anaplastic lymphoma kinase (ALK) inhibitory activity. The optimal compound I [R¹ = F; R² = EtSO; R³ = 4-methylpiperazin-1-yl; R⁴ = EtCONH; (II)] exhibited excellent antiproliferative activity against non-small cell lung cancer NCI-H2228 cells, which was better than that of Brigatinib and similar to Ceritinib. Mechanism study revealed that the compound II decreased the mitochondrial membrane potential and arrested NCI-H2228 cells in the G0/G1 phase, finally resulting in cellular apoptosis. It is interesting that the compound II could effectively inhibit the migration of NCI-H2228 cells and may be a promising leading compound for chemotherapy of metastatic cancer.

Bioorganic & Medicinal Chemistry Letters published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C11H8N2O2, Product Details of C7H5ClN2S.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Jeon, Yoon T. published the artcileIdentification of 1-{2-[4-chloro-1′-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4′-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y₁ antagonist as an antiplatelet agent, Synthetic Route of 31784-71-1, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(5), 1294-1298, database is CAplus and MEDLINE.

Spiropiperidine indoline-substituted diaryl ureas had been identified as antagonists of the P2Y₁ receptor. Enhancements in potency were realized through the introduction of a 7-hydroxyl substitution on the spiropiperidinylindoline chemotype. SAR studies were conducted to improve PK and potency, resulting in the identification of compound 3e, a potent, orally bioavailable P2Y₁ antagonist with a suitable PK profile in preclin. species. Compound 3e demonstrated a robust antithrombotic effect in vivo and improved bleeding risk profile compared to the P2Y₁₂ antagonist clopidogrel in rat efficacy/bleeding models.

Bioorganic & Medicinal Chemistry Letters published new progress about 31784-71-1. 31784-71-1 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorothiazolo[5,4-b]pyridin-2-amine, and the molecular formula is C6H4ClN3S, Synthetic Route of 31784-71-1.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Liu, Shuo published the artcileProgrammable and Reversible Regulation of Catalytic Hemin@MOFs Activities with DNA Structures, Computed Properties of 30931-67-0, the publication is Chemical Research in Chinese Universities (2020), 36(2), 301-306, database is CAplus.

Abstract: Metal-organic frameworks(MOFs)-based nanozyme plays an important role in biosensing, therapy and catalysis. In this study, the effects of single-stranded DNA(ssDNA) with programmable sequences and its complementary DNA(TDNA) on the intrinsic peroxidase-like activity of hemin loaded MOFs(UiO-66-₂), denoted as hemin@UiO-66-NH₂, were investigated. The hemin@UiO-66-₂ exhibited improved catalytic activity compared with free hemin. However, the catalytic activity is inhibited in the presence of ssDNA, as ssDNA can be adsorbed by MOFs and therefore protected the active sites from contact with substrates. Upon the addition of the T_DNA, double-stranded DNA(dsDNA) was formed and detached from the MOFs, resulting in the recovery of catalytic activity. Sequentially adding ssDNA or its complementary DNA strands can achieve the reversible regulation of the catalytic activity of MOFs nanozymes. Moreover, the DNA hybridization-based regulation was further applied to a cascaded catalytic system composed of the nanozyme, hemin@UiO-66-NH₂, and glucose oxidase. These nanozyme based programmable and reversibly regulated catalytic systems may have potential applications in future smart biosensing and catalysis systems.

Chemical Research in Chinese Universities published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C18H24N6O6S4, Computed Properties of 30931-67-0.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Zhang, Guohua published the artcileEthanol extracts from Cinnamomum camphora seed kernel: Potential bioactivities as affected by alkaline hydrolysis and simulated gastrointestinal digestion, COA of Formula: C18H24N6O6S4, the publication is Food Research International (2020), 109363, database is CAplus and MEDLINE.

The aim of the study was to evaluate the changes of potential bioactivities of ethanol extracts (EE) from Cinnamomum camphora seed kernel (CCSK) after alk. hydrolysis and simulated gastrointestinal digestion. The total phenolic and total flavonoid contents in EE decreased by 30.6%, 1%, 33% and 11.8% after hydrolysis and digestion, resp. The total saponins content decreased by 17% after hydrolysis while increased by 48% after digestion. The total condensed tannin contents increased by 70.3% and 17.2% after hydrolysis and digestion, resp. The 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), cupric ion reducing activity (CUPRAC), ferric reducing antioxidant power (FRAP) and metal chelating activity (MCA) were used to determine antioxidant activity. Overall, the changes of antioxidant activities by hydrolysis and digestion were consistent with the changes of their total phenolic and flavonoid contents. The α-amylase and α-glucosidase inhibitory activities in EE increased by 817% and 33.3% after digestion while decreased by 12.3% and 19% after hydrolysis, resp. Although the inhibitory activities of cholinesterase, tyrosinase and xanthine oxidase were decreased by hydrolysis and digestion, most of these activities were retained. These results showed that CCSK ethanol extracts had strong bioactivities and were reasonably stable to alkali and digestive enzymes.

Food Research International published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C20H17FO4S, COA of Formula: C18H24N6O6S4.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Zou, Yuke published the artcileNIR-Responsive Polyurethane Nanocomposites Based on PDA@FA Nanoparticles with Synergistic Antibacterial Effect, Recommanded Product: Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), the publication is Macromolecular Chemistry and Physics, database is CAplus.

At present, high-performance antibacterial polymer materials have attracted widespread attention, possessing huge application prospects in the fields of medical and biol. science, and packaging. In this work, polydopamine nanoparticles (PDA NPs) with photothermal ability and active sites are designed to adsorb fusidic acid (FA) mols. with targeted antibacterial capability; then, polydopamine@fusidic acid (PDA@FA) is introduced into the polyurethane (PU) to obtain multifunctional and antibacterial PU materials (PUDA@FA). The structures and morphologies of PDA NPs and PDA@FA are successfully characterized by Fourier transform-IR spectroscopy and SEM. With the introduction of PDA@FA, the nano-sized reinforcement not only greatly improves the mech. properties (tensile strength 19.31 MPa and toughness 10.6 MJ m^-3) of PU film but also due to the photothermal effect of PDA NPs and the antibacterial of FA, the scavenging activities of DPPH and ABTS reach 70-85% and 55-70%, resp. The antibacterial rate of Staphylococcus aureus reaches more than 99.9% and presents long-term antibacterial ability. In this way, this work provides new guidance for the preparation of high-performance PU materials with both antibacterial and anti-oxidation properties, broadening the application scope of antibacterial materials.

Macromolecular Chemistry and Physics published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C10H14O2, Recommanded Product: Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate).

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Khan, Takallum published the artcileSilica-Supported P₂O₅ as an Efficient Heterogeneous Catalyst for the One Pot Synthesis of 3-Amino-imidazo[2,1-b](1,3)benzothiazole under Green Conditions, HPLC of Formula: 95-24-9, the publication is Journal of Heterocyclic Chemistry (2019), 56(1), 11-17, database is CAplus.

The new approach involving the solid supported catalyst for the formation of C-N bond followed by cyclization has been reported. In this work we have reported a facile, efficient, and environment-friendly protocol for the synthesis of some new 3-amino-imidazo[2,1-b](1,3)benzothiazole derivatives by one-pot condensation of 2-aminobenzothiazole, indole-3-carbaldehyde, and aryl isocyanide in the presence of silica-supported P2O5 as a heterogeneous solid acid catalyst. The reaction was performed using conventional method under green conditions. The present approach offers the advantages of simple methodol., inexpensive acid catalyst, short reaction time, easy work up with excellent yield, simple purification and use of green solvent. All the newly synthesized compounds were characterized in details using phys. and chem. techniques such as m.p., 1H NMR, 13C NMR, and FTIR spectroscopy.

Journal of Heterocyclic Chemistry published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, HPLC of Formula: 95-24-9.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Li, Hui published the artcileSingle-Solution Doping Enabling Dominant Integer Charge Transfer for Synergistically Improved Carrier Concentration and Mobility in Donor-Acceptor Polymers, Related Products of thiazole, the publication is Advanced Functional Materials (2022), 32(14), 2110047, database is CAplus.

Chem. doping of donor-acceptor (D-A) polymers is essential for their usage in highly efficient optoelectronic devices. The crucial challenge remains to synergistically improve the carrier concentration and mobility of these polymers via a single solution doping method. Here, a D-A polymer, Pg₃2T-OTz is designed and synthesized, containing a weak-acceptor-strong-donor backbone with nonpolar (alkoxy) and polar (ethylene glycol) side chains. Pure integer charge transfer (ICT) is shown to occur in 2,3,5,6-tetrafluoro-tetracyanoquinodimethane (F4TCNQ)-doped D-A polymer at a low doping level. It is shown that the ordered edge-on orientations of ICT structures overcome the Coulomb interactions and endow a long-range hole delocalization, while few charge transfer complex states form in amorphous regions and bridge the crystalline ICT structures at high doping level, creating a network that sustains efficient charge transport. As a result, simultaneously high carrier concentration and high mobility are realized for F4TCNQ-doped Pg₃2T-OTz and thus a high elec. conductivity up to 550 S cm^-1 is approached, which is the highest value among any doped polymers via a single-solution doping process. This work demonstrates that the modulation of the acceptor strength combined with side-chain engineering is an effective mol. design strategy to promote both the doping efficiency and carrier transport property of D-A polymers.

Advanced Functional Materials published new progress about 2215018-37-2. 2215018-37-2 belongs to thiazole, auxiliary class Thiazoles, name is 4,4′-Bis(octyloxy)-2,2′-bis(trimethylstannyl)-5,5′-bithiazole, and the molecular formula is C28H52N2O2S2Sn2, Related Products of thiazole.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Ding, Hongyan published the artcileSKA3 promotes the proliferation, migration and invasion of endometrial carcinoma cells, Application of 6-Chlorobenzothiazol-2-ylamine, the publication is Chengdu Yixueyuan Xuebao (2021), 16(3), 293-298, database is CAplus.

Objective To investigate the effects of spindle and kinetochore associated complex subunit 3 (SKA3) on the proliferation, migration and invasion of endometrial carcinoma cells. Methods Real-time quant. polymerasechain reaction (RT-qPCR) and Western blotting were used to detect the levels of SKA3 mRNA and protein expression in endometrial epithelial cells HEECs and endometrial carcinoma cells KLE, JEC and Ishikawa cells. And the Ishikawa cells with the highest expression level were selected for subsequent research. Ishikawa cells were divided into three groups. In the control group, Ishikawa cells were cultured normally. In the si-SKA3 group, 50 nmol/L siRNA-SKA3 was transfected into Ishikawa cells according to liposome 2000 instructions. In the NC group, 50 nmol/L siRNA-NC was transfected into Ishikawa cells according to liposome 2000 instructions. Cell proliferation was detected by cell counting kit-8 (CCK8) and clonal formation assay. Cell invasion and migration were detected by Transwell and scratch assay. And protein expression of CyclinD1, MMP-2, AKT, and p-AKT were detected by Western blotting. Results Compared with the HEECs of endometrial epithelial cells, the expression levels of SKA3 mRNA and protein in each endometrial carcinoma cell line were significantly increased (P<0.05). After interference with SKA3 expression, the proliferation and invasion ability of Ishikawa cells were decreased, the width of scratches were enlarged, and the protein expression of CyclinD1 and MMP-2 were significantly decreased (P<0.05). Compared with the control group and the NC group, the expression of AKT protein in si-SKA3 group was not significantly changed (P>0.05), while the expression of p-AKT protein decreased (P<0.05). Conclusion Interference with SKA3 can inhibit the proliferation, migration and invasion of Ishikawa cells of endometrial carcinoma, of which the mechanism may be related to the inhibition of SKA3 on PI3K/AKT signaling pathway.

Chengdu Yixueyuan Xuebao published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Application of 6-Chlorobenzothiazol-2-ylamine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Sun, Mimi published the artcileA Bendable Biofuel Cell-Based Fully Integrated Biomedical Nanodevice for Point-of-Care Diagnosis of Scurvy, COA of Formula: C18H24N6O6S4, the publication is ACS Sensors (2021), 6(1), 275-284, database is CAplus and MEDLINE.

Fully integrated nanodevices that allow the complete functional implementation without an external accessory or equipment are deemed to be one of the most ideal and ultimate goals for modern nanodevice design and construction. In this work, we demonstrate the first example of a bendable biofuel cell (BFC)-based fully integrated biomedical nanodevice with simple, palm-sized, easy-to-carry, pump-free, cost-saving, and easy-to-use features for the point-of-care (POC) diagnosis of scurvy from a single drop of untreated human serum (down to 0.2μL) by integrating a bendable and disposable vitamin C/air microfluidic BFC (micro-BFC) (named iezCard) for self-powered vitamin C biosensing with a custom mini digital LED voltmeter (named iezBox) for signal processing and transmission, along with a ”built-in” biocomputing BUFFER gate for intelligent diagnosis. Under the simplicity- and practicability-oriented idea, a cost-effective strategy (e.g., biomass-derived hierarchical micro-mesoporous carbon aerogels, screen-printed technique, a single piece of Kimwipes paper, LED display, and universal components) was implemented for nanodevice design rather than any top-end or pricey method (e.g., photolithog./electron-beam evaporation, peristaltic pump, wireless system, and 3D printing technique), which enormously reduces the cost of feedstock down to ~USD 2.55 per integrated kit including a disposal iezCard (~USD 0.08 per test) and a reusable iezBox (~USD 2.47 for large-scale tests). These distinctive and attractive features allow such a fully integrated biomedical nanodevice to fully satisfy the basic requirements for POC diagnosis of scurvy from a single drop of raw human serum and make it particularly appropriate for resource-poor settings, where there is a lack of medical facilities, funds, and qualified personnel.

ACS Sensors published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C10H12F6N4O6PdS2, COA of Formula: C18H24N6O6S4.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica