Day: October 11, 2022

Lin, Xuexiang; Liu, Xiao-Yu; Zhang, Bo; Qin, Ai-Qing; Hui, Kwok-Min; Shi, Kevin; Liu, Yang; Gabriel, Don; Li, X. James published the artcile< A rapid influenza diagnostic test based on detection of viral neuraminidase activity>, Electric Literature of 2591-17-5, the main research area is neuraminidase enzyme assay influenza diagnosis.

Current methods used for diagnosis of acute infection of pathogens rely on detection of nucleic acids, antigens, or certain classes of antibodies such as IgM. Here we report a virus enzyme assay as an alternative to these methods for detection of acute viral infection. In this method, we used a luciferin derivative as the substrate for detection of the enzyme activity of influenza viral neuraminidase as a means for diagnosis of influenza. The resulting com. test, the qFLU Dx Test, uses a different supply chain that does not compete with those for the current tests. The assay reagents were formulated as a master mix that accommodated both the neuraminidase and luciferase reactions, thereby enabling rapid and prolonged production of stable light signal in the presence of influenza virus in the sample. The assay was evaluated using depository throat swab specimens. As expected, the assay exhibited similar detection rates for all influenza types and subtypes except for A(H7N9), which exhibited lower detection rate due to lower viral titer in the specimens. When throat swab specimens were diluted with the sample buffer of the test kit and tested with the qFLU Dx Test. The sensitivity and specificity were 82.41% (95% confidence interval: 79.66-85.84%) and 95.39% (95% confidence interval: 94.32-96.46%), resp., for these diluted specimens in comparison to a real-time polymerase chain reaction assay. The uniqueness of the qFLU Dx Test as an enzymic assay makes it highly complementary with currently available methods.

Scientific Reports published new progress about Diagnosis. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Electric Literature of 2591-17-5.

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

Sanichar, Randy; Carroll, Ciaran; Kimmis, Ryan; Reiz, Bela; Vederas, John C. published the artcile< Dess-Martin periodinane oxidative rearrangement for preparation of α-keto thioesters>, HPLC of Formula: 171877-39-7, the main research area is Dess Martin periodinane oxidative rearrangement alpha keto thioester preparation; keto thioester preparation oxidation beta hydroxy thioester.

A Dess-Martin Periodinane (DMP) mediated oxidative rearrangement reaction was uncovered. The reaction proceeds via oxidation of a β-hydroxy thioester to a β-keto thioester, followed by an α-hydroxylation and then further oxidation to form a vicinal thioester tricarbonyl. This product then rearranges, extruding CO2, to form an α-keto product. The mechanism of the rearrangement was elucidated using 13C labeling and anal. of the intermediates as well as the products of the reaction. This efficient process allows for easy preparation of α-keto thioesters which are potential intermediates in the synthesis of pharmaceutically important heterocyclic scaffolds such as quinoxalinones.

Organic & Biomolecular Chemistry published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, HPLC of Formula: 171877-39-7.

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

Ford, Kevin A.; Gulevich, Alexander G.; Swenson, Tami L.; Casida, John E. published the artcile< Neonicotinoid Insecticides: Oxidative Stress in Planta and Metallo-oxidase Inhibition>, SDS of cas: 1003-32-3, the main research area is neonicotinoid insecticide oxidative stress plant metallooxidase inhibition.

Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean (Glycine max) seedlings assayed with the 3,3′-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.

Journal of Agricultural and Food Chemistry published new progress about Chlorosis (plant). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, SDS of cas: 1003-32-3.

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

Huang, Gaochao; Shrestha, Ruben; Jia, Kaimin; Geisbrecht, Brian V.; Li, Ping published the artcile< Enantioselective Synthesis of Dilignol Model Compounds and Their Stereodiscrimination Study with a Dye-Decolorizing Peroxidase>, Synthetic Route of 171877-39-7, the main research area is dilignol model compound enantioselective preparation surface plasmon resonance TcDyP.

A four-step enantioselective approach was developed to synthesize anti (1R,2S)-I and (1S,2R)-I containing a β-O-4 linkage in good yields. A significant difference was observed for the apparent binding affinities of four stereospecific lignin model compounds with TcDyP by surface plasmon resonance, which was not translated into a significant difference in enzyme activities. The discrepancy may be attributed to the conformational change involving a loop widely present in DyPs upon H2O2 binding.

Organic Letters published new progress about Diastereoselective synthesis. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Synthetic Route of 171877-39-7.

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

Chen, Qi-Yin; Chaturvedi, Pravin R.; Luesch, Hendrik published the artcile< Process development and scale-up total synthesis of largazole, a potent class I histone deacetylase inhibitor>, COA of Formula: C12H18N2O4S, the main research area is macrocyclic depsipeptide natural product largazole total enantioselective synthesis; largazole anticancer agent histone deacetylase inhibitor drug design; hydrolysis fragment condensation Seebach procedure formylation methylation safety; Aldol condensation enzymic resolution peptide coupling macrocyclization cross metathesis.

Herein we describe the research and development of the process for the scale-up total synthesis of largazole, a potent class I selective histone deacetylase (HDAC) inhibitor, a potential anticancer agent and also useful for the treatment of other disorders where transcriptional reprogramming might be beneficial. The synthetic route and conditions for each fragment and final product were modified and optimized to make them suitable for larger-scale synthesis. With the process we developed, hundreds of grams of each fragment and decagrams of final product largazole were synthesized in good to excellent yields. The final target largazole was obtained in 21% overall yield over eight steps based on the longest sequence with over 95% HPLC purity.

Organic Process Research & Development published new progress about Aldol condensation. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, COA of Formula: C12H18N2O4S.

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

de Souza, Daniel Rangel; Silva, Jaqueline Rodrigues; Moreira, Ariele; Viviani, Vadim R. published the artcile< Biosensing firefly luciferin synthesis in bacteria reveals a cysteine-dependent quinone detoxification route in Coleoptera>, Application of C11H8N2O3S2, the main research area is .

Abstract: Luciferin biosynthetic origin and alternative biol. functions during the evolution of beetles remain unknown. We have set up a bioluminescent sensing method for luciferin synthesis from cysteine and benzoquinone using E. coli and Pichia pastoris expressing the bright Amydetes vivianii firefly and P. termitilluminans click beetle luciferases. In the presence of D-cysteine and benzoquinone, intense bioluminescence is quickly produced, indicating the expected formation of D-luciferin. Starting with L-cysteine and benzoquinone, the bioluminescence is weaker and delayed, indicating that bacteria produce L-luciferin, and then racemize it to D-luciferin in the presence of endogenous esterases, CoA and luciferase. In bacteria the p-benzoquinone toxicity (IC50 ∼ 25 μM) is considerably reduced in the presence of cysteine, maintaining cell viability at 3.6 mM p-benzoquinone concomitantly with the formation of luciferin. Transcriptional anal. showed the presence of gene products involved with the sclerotization/tanning in the photogenic tissues, suggesting a possible link between these pathways and bioluminescence. The lack of two enzymes involved with the last steps of these pathways, indicate the possible accumulation of toxic quinone intermediates in the lanterns. These results and the abundance of cysteine producing enzymes suggest that luciferin first appeared as a detoxification byproduct of cysteine reaction with accumulated toxic quinone intermediates during the evolution of sclerotization/tanning in Coleoptera.

Scientific Reports published new progress about 2591-17-5. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application of C11H8N2O3S2.

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

Robertson, Mark J.; Hadzic, Gordana; Ambrus, Joseph; Pome, D. Yuri; Hyde, Emily; Whiting, Ainslie; Mariana, Anna; von Kleist, Lisa; Chau, Ngoc; Haucke, Volker; Robinson, Phillip J.; McCluskey, Adam published the artcile< The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity>, SDS of cas: 10574-69-3, the main research area is dynamin GTPase inhibitor rhodanine analog preparation SAR; Knoevengal condensation; dynamin inhibition; rhodanine.

Six focused rhodanine-based libraries, 60 compounds in total, were synthesized and evaluated as potential dynamin I GTPase inhibitors. Twenty-six were more potent than the lead compound with 13 returning IC50 values ≤10 μM, making the Rhodadyn series among the most active dynamin inhibitors reported. Two analogs were highly effective at blocking receptor-mediated endocytosis: C10 and D10 (I) with IC50(RME) = 7.0 ± 2.2 and 5.9 ± 1.0 μM, resp. These compounds are equipotent with the best reported in-cell dynamin inhibitors.

ACS Medicinal Chemistry Letters published new progress about Drug targets (endocytosis). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, SDS of cas: 10574-69-3.

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

da Silva, Monize M.; de Camargo, Mariana S.; Castelli, Silvia; de Grandis, Rone A.; Castellano, Eduardo E.; Deflon, Victor M.; Cominetti, Marcia R.; Desideri, Alessandro; Batista, Alzir A. published the artcile< Ruthenium(II)-mercapto complexes with anticancer activity interact with topoisomerase IB>, Safety of 4,5-Dihydrothiazole-2-thiol, the main research area is rutheniumII mercapto anticancer activity topoisomerase IB lung liver cancer.

Herein we present four new ruthenium(II) complexes: [Ru(mtz)2(dppb)] (1), [Ru(mmi)2(dppb)] (2), [Ru(dmp)2(dppb)] (3), and [Ru(mpca)2(dppb)] (4), where mtz = 2-mercaptothiazoline; mmi = 2-mercapto-1-methyl-imidazole; dmp = 4,6-diamino-2-mercaptopyrimidine; mpca = 6-mercaptopyridine-3-carboxylic acid; dppb = 1,4-bis(diphenylphosphino)butane. In vitro cell culture experiments revealed cytotoxic activity for complexes 2, 3 and 4 against MCF-7 (breast, non-invasive), MDA-MB-231 (breast, invasive), A549 (lung), DU-145 (prostate) and HepG2 (liver) tumor cells, in some cases lower than the half maximal inhibitory concentration (IC50) for the reference drug (cisplatin). The DNA (DNA) interactions studied by viscosity measurements, gel electrophoresis and square-wave voltammetry indicated that the DNA binding affinity primarily occurs through non-covalent interactions. Only complex 2 was able to fully inhibit the DNA supercoiled relaxation mediated by human topoisomerase IB (Top IB). The anal. indicates that complex 2 inhibits the cleavage and the reconnection steps of the catalytic cycle, being both a poison and a catalytic inhibitor.

Journal of the Brazilian Chemical Society published new progress about Antitumor agents. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Safety of 4,5-Dihydrothiazole-2-thiol.

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

Fan, Di; Wang, Ting; Hu, Jinhui; Zhou, Lin; Zhou, Jiahong; Wei, Shaohua published the artcile< Plasmid DNA-Based Bioluminescence-Activated System for Photodynamic Therapy in Cancer Treatment>, Electric Literature of 2591-17-5, the main research area is cervical cancer plasmid DNA bioluminescence photodynamic therapy; hypericin; luciferase; photodynamic therapy; plasmid DNA; singlet oxygen.

The low depth of tissue penetration by therapeutic light sources severely restricts photodynamic therapy (PDT) in treating deep-seated tumors. Using a luciferase/D-luciferin bioluminescence system to artificially create internal light sources in cells instead of external light sources is an effective means of solving the above problems. However, high-efficiency bioluminescence requires a higher concentration of luciferase in the cell, which poses a considerable challenge to the existing system of enzyme loading, delivery, activity and retention of drugs, and dramatically increases the cost of treatment. We loaded the substrate D-luciferin, and the photosensitizer hypericin into a polyethyleneimine (PEI)-modified nano-calcium phosphate (CaP) to solve this problem. Subsequently, the plasmid DNA containing the luciferase gene was loaded onto it using the high-d. pos. charge characteristic of PEI from the nanodrug (denoted DHDC). After the DHDC enters the tumor cell, it collapses and releases the plasmid DNA, which uses the intracellular protein synthesis system to continuously and massively express luciferase. Using endogenous ATP, Mg2+, and O2 in cells, luciferase oxidizes D-luciferin and produces luminescence. The luminescence triggers hypericin excitation to generate ROS and kill cancer cells. This study provides a new strategy for the application of bioluminescence in PDT treatment.

ChemMedChem published new progress about Antitumor agents. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Electric Literature of 2591-17-5.

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

Yang, Ping; Luo, Jia-Bao; Wang, Zi-Zhou; Zhang, Li-Lei; Xie, Xiao-Bao; Shi, Qing-Shan; Zhang, Xin-Guo published the artcile< Synthesis and in vitro antibacterial activity of N-acylarylhydrazone-ciprofloxacin hybrids as novel fluoroquinolone derivatives>, Recommanded Product: Thiazole-5-carboxyaldehyde, the main research area is acylarylhydrazone ciprofloxacin hybrid diastereoselective preparation mol docking antibacterial.

Twelve novel fluoroquinolone derivatives I [R = 3,4-di-HOC6H3, 2,3-di-FC6H3, 2,5-di-FC6H3, etc.] were rationally designed and synthesized by introducing N-acylarylhydrazone to the C-7 position of ciprofloxacin. Antibacterial evaluation revealed that compound I [R = (E)-2,6-di-FC6H3CH=CH] was over 4-folds more potent than ciprofloxacin against S. aureus, with a MIC value ≤0.125μg/mL. Compound I [R = (E)-4-BrC6H4CH=CH] showed activity against methicillin-resistant S. aureus (MRSA) with a MIC value of 32μg/mL. Time-killing assays showed that compound I [R = (E)-4-BrC6H4CH=CH] eradicated S. aureus in 4 h and E. coli in 2 h. Compound I [R = (E)-4-BrC6H4CH=CH] had a high affinity toward DNA topoisomerase IV, with a least binding energy of -9.9 kcal/mol, which was better than ciprofloxacin (-8.0 kcal/mol). The binding modes of compound I [R = (E)-4-BrC6H4CH=CH] to DNA topoisomerase IV differed from that of ciprofloxacin. Mol. dynamics simulation results support that the interaction between the receptor 3rae and the compound I [R = (E)-4-BrC6H4CH=CH] was stable. Besides, cytotoxicity and hemolysis assays demonstrated that compound I [R = (E)-4-BrC6H4CH=CH] and I [R = (E)-2,6-di-FC6H3CH=CH] had negligible risks of toxic effects.

Journal of Molecular Structure published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Recommanded Product: Thiazole-5-carboxyaldehyde.

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