Month: November 2021

In 2019 BIOORGAN MED CHEM published article about CARFILZOMIB; DESIGN in [Lei, Meng; Miao, Hang; Feng, Huayun] Nanjing Forestry Univ, Coll Sci, 159 Longpan Rd, Nanjing 210037, Jiangsu, Peoples R China; [Zhang, Haoyang; Du, Xiao; Zhou, Hui; Wang, Xueyuan; Zhu, Yongqiang] Nanjing Normal Univ, Coll Life Sci, 1 Wenyuan Rd, Nanjing 210046, Jiangsu, Peoples R China; [Wang, Jia; Shi, Jingmiao; Liu, Zhaogang; Zhu, Yongqiang] Jiangsu Chia Tai Fenghai Pharmaceut Co Ltd, 9 Weidi Rd, Nanjing 210046, Jiangsu, Peoples R China; [Shen, Jian] Nanjing Normal Univ, Coll Chem & Mat Sci, 1 Wenyuan Rd, Nanjing 210046, Jiangsu, Peoples R China in 2019, Cited 21. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Recommanded Product: 98-97-5

A series of novel tetrapeptidyl epoxyketone inhibitors of 20S proteasome was designed and synthesized. To fully understand the SAR, various groups at R-1, R-2, R-3, R-4 and R-5 positions, including aromatic and aliphatic substituents were designed, synthesized and biologically assayed. Based on the enzymatic results, seven compounds were selected to evaluate their cellular activities and soluble compound 36 showed strong potency against human multiple myeloma (MM) cell lines. Microsomal stability results indicated that compound 36 was more stable in mice, rat and human microsomes than marketed carfilzomib. The in vivo activities of this compound were evaluated with the xenograft mice models of MM cell lines ARH77 and RPMI-8226 with luciferase expression and the T/C value of the two models were 49.5% and 37.6%, respectively. To evaluate the potential cardiovascular toxicity, inhibition of hERG ion channel in HEK293 cells by compound 36 and carfilzomib was carried out. The results indicated that 36 had no binding affinity for the hERG ion channel while carfilzomib could bind it with IC50, of 92.1 mu M.

Recommanded Product: 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Lei, M; Zhang, HY; Miao, H; Du, X; Zhou, H; Wang, J; Wang, XY; Feng, HY; Shi, JM; Liu, ZG; Shen, J; Zhu, YQ or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

I found the field of Environmental Sciences & Ecology very interesting. Saw the article Zirconium-Containing Organic-Inorganic Nanohybrid as a Highly Efficient Catalyst for the Selective Synthesis of Biomass-Derived 2,5-Dihydroxymethylfuran in Isopropanol published in 2020. Quality Control of Pyrazine-2-carboxylic acid, Reprint Addresses Hu, L; Xu, JX (corresponding author), Huaiyin Normal Univ, Jiangsu Collaborat Innovat Ctr Reg Modern Agr & E, Sch Chem & Chem Engn, Jiangsu Key Lab Biomass Based Energy & Enzyme Tec, Huaian 223300, Peoples R China.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

By the simple assembly of zirconium tetrachloride and diethylenetriaminepentaacetic acid (DTPA), a new acid-base bifunctional zirconium-containing organic-inorganic nanohybrid catalyst (Zr-DTPA) was successfully prepared in this work, and then used for the catalytic transfer hydrogenation (CTH) of biomass-derived 5-hydroxymethylfurfural (HMF) into 2,5-dihydroxymethylfuran (DHMF) using isopropanol as the in situ hydrogen donor and reaction solvent. Satisfactorily, 98.7% HMF conversion and 95.2% DHMF yield could be achieved in 4 h at a moderate reaction temperature of 140 degrees C. After systematic studies, this excellent catalytic activity was proved to be mainly ascribed to the synergistic effect of Lewis-acidic sites (Zr4+) and Lewis-basic sites (O2- and N) with higher strengths and contents. Meanwhile, Zr-DTPA could be readily separated by filtration, when it was repeatedly used 5 recycles, its catalytic activity was not obviously changed, demonstrating that Zr-DTPA had good heterogeneity and reusability. More importantly, Zr-DTPA could also be employed to effectively catalyze the CTH of 5-methylfurfural, furfural, levulinic acid, ethyl levulinate and cyclohexanone into the corresponding products with high yields, indicating that it showed a superior universality for the selective hydrogenation of various biomass-derived carbonyl compounds.Graphical Abstract

Welcome to talk about 98-97-5, If you have any questions, you can contact Hu, L; Liu, S; Song, J; Jiang, YT; He, AY; Xu, JX or send Email.. Quality Control of Pyrazine-2-carboxylic acid

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Product Details of 98-97-5. Recently I am researching about ANTITUMOR-ACTIVITY; QUINOXALINE DERIVATIVES; THIOPHENE DERIVATIVES; CRYSTAL-STRUCTURE; TUMOR-CELLS; ANTICANCER; CYTOTOXICITY; COPPER(II); INHIBITORS; COMPLEXES, Saw an article supported by the National Key Research and Development Program of China [2017YFD0600706]; Sate Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University) [CMEMR2017-B06]. Published in TAYLOR & FRANCIS LTD in ABINGDON ,Authors: Zhao, FY; Sun, X; Lu, W; Xu, L; Shi, JZ; Yang, SL; Zhou, MY; Su, F; Lin, F; Cao, FL. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Several dehydroabietylamine derivatives containing heterocyclic moieties such as thiophene and pyrazine ring were successfully synthesized. The antiproliferative activities of these thiophene-based Schiff-bases, thiophene amides, and pyrazine amides were investigated in vitro against Hela (cervix), MCF-7 (breast), A549 (lung), HepG2 (liver), and HUVEC (umbilical vein) cells by MTT assay. The toxicity of L-1-L-10 (IC50 = 5.92- >100 mu M) was lower than L-0 (1.27 mu M) and DOX (4.40 mu M) in every case. Compound L-1 had higher anti-HepG2 (0.66 mu M), anti-MCF-7 (5.33 mu M), and anti-A549 (2.11 mu M) and compound L-3 had higher anti-HepG2 (1.63 mu M) and anti-MCF-7 (2.65 mu M) activities. Both of these compounds were recognized with high efficiency in apoptosis induction in HepG2 cells and intercalated binding modes with DNA. Moreover, with average IC50 values of 0.66 and 5.98 mu M, L-1 was nine times more effective at suppressing cultured HepG2 cells viability than normal cells (SI = 9). The relative tumor proliferation rate (T/C) was 38.6%, the tumor inhibition rate was up to 61.2%, which indicated that L-1 had no significant toxicity but high anti-HepG2 activity in vivo. Thus, it may be a potential antiproliferation drug with nontoxic side effects.

Product Details of 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Zhao, FY; Sun, X; Lu, W; Xu, L; Shi, JZ; Yang, SL; Zhou, MY; Su, F; Lin, F; Cao, FL or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Kelesoglu, A; Sigircik, G; Yildiz, R; Dehri, I in [Kelesoglu, Aysen; Sigircik, Gokmen; Dehri, Ilyas] Cukurova Univ, Fac Sci & Letters, Chem Dept, Adana, Turkey; [Yildiz, Resit] Mardin Artuklu Univ, Fac Hlth Sci, Dept Nutr & Dietet, Mardin, Turkey; [Yildiz, Resit] Mardin Artuklu Univ, Cent Res Lab, Mardin, Turkey published Inhibition efficiency of pyrazinecarboxylic acid on mild steel in acidic environment in 2021, Cited 62. Name: Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Pyrazinecarboxylic acid (PCA) was examined as a potential corrosion inhibitor for mild steel (MS) in 0.5 M HCl environment. The methods of electrochemical impedance spectroscopy (EIS), linear polarization resistance (LPR), as well potentiodynamic (PD) polarization were utilized. Furthermore, atomic force microscopy (AFM) and quantum chemical calculations were utilized. PD polarization curves demonstrated that PCA exhibited mixed inhibitor behavior. Scanning electron microscopy (SEM) offered the creation of an adsorptive layer on the surface of MS which prevented the steel against corrosive specimens. Furthermore, density functional theory (DFT) presented good agreement with electrochemical experimental results. The adsorption equilibrium constant (k(ads)) value was calculated to be 3.704 x 10(4) M-1 which was related to a high proportion of inhibitor on the surface. In the presence of 1.0 mM PCA, inhibition efficiency was determined as 95.2% from EIS results.

Name: Pyrazine-2-carboxylic acid. Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

An article Total Synthesis of Echinomycin and Its Analogues WOS:000538848600034 published article about PHASE-II TRIAL; ORGANIC SULFUR CHEMISTRY; QUINOXALINE ANTIBIOTICS; TRIOSTIN; HYPOXIA; DESULFURIZATION; DEPSIPEPTIDES; QUINOMYCIN; PATHWAY in [Ichikawa, Satoshi] Hokkaido Univ, Global Inst Collaborat Res & Educ GI CoRE, Fac Pharmaceut Sci, Ctr Res & Educ Drug Discovery, Sapporo, Hokkaido 0600812, Japan; [Ichikawa, Satoshi] Hokkaido Univ, Global Inst Collaborat Res & Educ GI CoRE, Global Stn Biostofaces & Drug Discovery, Sapporo, Hokkaido 0600812, Japan; [Kojima, Keita; Yakushiji, Fumika; Katsuyama, Akira] Hokkaido Univ, Fac Pharmaceut Sci, Sapporo, Hokkaido 0600812, Japan; [Yakushiji, Fumika; Katsuyama, Akira] Hokkaido Univ, Fac Pharmaceut Sci, Ctr Res & Educ Drug Discovery, Sapporo, Hokkaido 0600812, Japan in 2020, Cited 32. Product Details of 98-97-5. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

The first total synthesis of echinomycin (1) was accomplished by featuring the late-stage construction of the thioacetal moiety via Pummerer rearrangement and simultaneous cyclization, as well as two-directional elongation of the peptide chains to construct a C2-symmetrical bicyclic octadecadepsipeptide bridged with a sulfide linkage. This strategy can be applicable to a variety of echinomycin analogues.

Product Details of 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Kojima, K; Yakushiji, F; Katsuyama, A; Ichikawa, S or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recently I am researching about ONE-POT SYNTHESIS; MULTICOMPONENT REACTIONS; POSTCONDENSATION MODIFICATIONS; BUILDING-BLOCKS; SOLID-STATE; ISOCYANIDE; HEXAMETHYLENETETRAMINE; CHEMISTRY; AMMONIA; MECHANISM, Saw an article supported by the CNPqConselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPQ); CAPESCoordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES); FAP-DFFundacao de Apoio a Pesquisa do Distrito Federal (FAPDF); Instituto de Quimica, Universidade de Brasilia. Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Rosalba, TPF; Kas, SSA; Sampaio, ABS; Salvador, CEM; Andrade, CKZ. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid. Product Details of 98-97-5

Ugi reactions are still a challenge when the concomitant use of ammonia and formaldehyde is required. Herein, we propose a strategy to overcome this challenge using hexamethylenetetramine (HMTA) as a singular key for the employment of these two simple starting materials in the Ugi reaction. Acylaminoacetamide derivatives were prepared in good to excellent yields by this new methodology. The scope and optimization of the reaction conditions were investigated. This novel methodology was successfully applied in the synthesis of two different diketopiperazines (DKPs) using the Ugi/Deprotection+Activation/Cyclization (UDAC) method. A continuous flow approach was also used in this methodology.

Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.. Product Details of 98-97-5

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

An article Exploring the Pyrazinamide Drug Resistance Mechanism of Clinical Mutants T370P and W403G in Ribosomal Protein S1 of Mycobacterium tuberculosis WOS:000465644500029 published article about MOLECULAR-DYNAMICS; SHAPE COMPLEMENTARITY; BINDING; DOCKING; SYSTEM; IDENTIFICATION; TRANSLATION; CONSTRAINTS; MUTATION; INSIGHT in [Rehman, Ashfaq Ur; Liu, Hao; Chen, Hai-Feng] Shanghai Jiao Tong Univ, Sch Life Sci & Biotechnol, Natl Expt Teaching Ctr Life Sci & Biotechnol, State Key Lab Microbial Metab,Dept Bioinformat &, Shanghai 200240, Peoples R China; [Chen, Hai-Feng] Shanghai Ctr Bioinformat Technol, Shanghai 200235, Peoples R China; [Khan, Muhammad Tahir; Malik, Shaukat Iqbal] Capital Univ Sci & Technol, Dept Bioinformat & Biosci, Islamabad 44000, Pakistan; [Rehman, Ashfaq Ur; Wadood, Abdul] Abdul Wali Khan Univ Marden, Dept Biotechnol, Mardan 23200, Pakistan in 2019, Cited 62. Name: Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Pyrazinamide (PZA) is an essential first line antitubercular drug, which plays a crucial role in tuberculosis treatment. The PZA, which is considered as a pro-drug needs an enzyme of mycobacterial pyrazinamidase (PZase) for its conversion into an active form pyrazinoic acid. Further, this active form of PZA inhibits the ribosomal proteins Si, which facilitates the transfer-mRNA complex formation throughout the translation. The spontaneous mutations in RpsA have been found to be associated with PZA drug resistance. However, the drug resistance mechanism is still unclear. Furthermore, there is no such information available about the structural dynamics of RpsA protein because of mutations that confer Pyrazinoic acid resistance. Moreover, a total of 18 clinical PZA-resistant isolates were investigated and found to be pncA(WT), which allowed exploration of the resistance mechanism of RpsA in the mutated state. Samples were repeated for the drug susceptibility testing followed by RpsA gene sequencing. A total of 11 clinical isolates harbored a total of 15 mutations. Almost half of the total strains (7/15) were observed to be in the conserved region of RpsA and known as Mycobacterium tuberculosis C-terminal domain. In the current study, (2/7) mutation T370P (mutant 1) and W403G (mutant 2) were explored to ensure the RpsA resistance mechanism through essential dynamics simulation. The essential dynamics study results revealed that the distal loop mutations drastically altered the conformation of RpsA both in the absence () and presence (+) of pyrazinoic acid drug for two reasons: (1) dramatic alteration or reduction in the binding pattern of pyrazinoic acid with active site residues observed and (2) a clear image of the opening and closing switching mechanism was seen upon the distal site mutation on nearby 3(10)-helixes beside the pyrazinoic acid binding site. This switch was found to consistently remain closed only in wild type systems, while it was open in the mutant systems. We called such distance impact an allosteric effect. The overall mechanistic investigations will provide useful information behind drug resistance for better understanding to manage tuberculosis.

Name: Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Rehman, AU; Khan, MT; Liu, H; Wadood, A; Malik, SI; Chen, HF or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recently I am researching about MYCOBACTERIUM-TUBERCULOSIS; CATALASE-PEROXIDASE; SUSCEPTIBILITY; ARTEMISININ; ANTIMALARIAL; RESISTANCE; KATG, Saw an article supported by the CSIR Thematic Program Fund; South African Medical Research CouncilUK Research & Innovation (UKRI)Medical Research Council UK (MRC) [MRC-RFA-UFSP-01-2013]; SAMRCUK Research & Innovation (UKRI)Medical Research Council UK (MRC). Recommanded Product: 98-97-5. Published in BENTHAM SCIENCE PUBL LTD in SHARJAH ,Authors: van der Westhuyzen, CW; Haynes, RK; Panayides, JL; Wiid, I; Parkinson, CJ. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Background: With few exceptions, existing tuberculosis drugs were developed many years ago and resistance profiles have emerged. This has created a need for new drugs with discrete modes of action. There is evidence that tuberculosis (like other bacteria) is susceptible to oxidative pressure and this has yet to be properly utilised as a therapeutic approach in a manner similar to that which has proven highly successful in malaria therapy. Objective: To develop an alternative approach to the incorporation of bacterial siderophores that results in the creation of antitubercular peroxidic leads for subsequent development as novel agents against tuberculosis. Methods: Eight novel peroxides were prepared and the antitubercular activity (H(37)Rv) was compared to existing artemisinin derivatives in vitro. The potential for toxicity was evaluated against the L6 rat skeletal myoblast and HeLa cervical cancer lines in vitro. Results: The addition of a pyrimidinyl residue to an artemisinin or, preferably, a tetraoxane peroxidic structure results in antitubercular activity in vitro. The same effect is not observed in the absence of the pyrimidine or with other heteroaromatic substituents. Conclusion: The incorporation of a pyrimidinyl residue adjacent to the peroxidic function in an organic peroxide results in anti-tubercular activity in an otherwise inactive peroxidic compound. This will be a useful approach for creating oxidative drugs to target tuberculosis.

Welcome to talk about 98-97-5, If you have any questions, you can contact van der Westhuyzen, CW; Haynes, RK; Panayides, JL; Wiid, I; Parkinson, CJ or send Email.. Recommanded Product: 98-97-5

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

An article Pantoprazole Derivatives: Synthesis, Urease Inhibition Assay and In Silico Molecular Modeling Studies WOS:000528045700025 published article about HELICOBACTER-PYLORI; BIOISOSTERIC TRANSFORMATIONS; TRIPLE THERAPY; PATHOGENESIS; METAANALYSIS; OXADIAZOLES; PREDICTION in [Azizian, Homa] Iran Univ Med Sci, Sch Pharm, Dept Med Chem, Int Campus, Tehran, Iran; [Esmailnejad, Atefeh; Fathi Vavsari, Vaezeh; Balalaie, Saeed] KN Toosi Univ Technol, Peptide Chem Res Ctr, POB 15875-4416, Tehran, Iran; [Mahernia, Shabnam; Amanlou, Massoud] Univ Tehran Med Sci, TIPS, Drug Design & Dev Res Ctr, Tehran, Iran; [Balalaie, Saeed] Kermanshah Univ Med Sci, Med Biol Res Ctr, Kermanshah, Iran in 2020, Cited 42. SDS of cas: 98-97-5. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

A number of pantoprazole derivatives were synthesized and screened for their urease inhibitory properties. Some of them showed potent inhibitions against jack bean urease. All compounds showed varying degree of IC50 in the range of 25.85 to 181 mu Mol as compared to standard acetohydroxamic acid (AHA) (100 +/- 2.02 mu Mol). Derivatives bearing 5-aryl-1,3,4-oxadiazole ring substitutions (aryl= pyrazyl, pyridyl and phenyl) were found to be more potent inhibitors than AHA and pantoprazole. The most promising compound, 2-((3,4-dimethoxypyridin-2-yl)methylthio)-5-(pyrazin-2-yl)-1,3,4-oxadiazole 12, with IC50 value of 25.85 +/- 1.21 showed remarkable urease inhibition activity. In silico molecular modeling investigation performed to rationalize the possible binding interaction and ADME properties of compounds over the active site of urease enzyme. The induced fit docking study showed that compound 12 interacted with conserved residues His593 and Arg609 located at the mouth of the urease active site flap and are essential for enzyme catalytic activity. These target compounds could be further studied as a lead skeleton for discovery of novel urease inhibitors.

SDS of cas: 98-97-5. Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In 2020 ORG LETT published article about CARBOXYLIC-ACIDS; HYDROAMINATION; ISOTHIOCYANATES; CHEMISTRY; FACILE; AMINO in [Derasp, Joshua S.; Barbera, Erica A.; Seguin, Nieve R.; Brzezinski, David D.; Beauchemin, Andre M.] Univ Ottawa, Ctr Catalysis Res & Innovat, Dept Chem & Biomol Sci, Ottawa, ON K1N 6N5, Canada in 2020, Cited 51. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Safety of Pyrazine-2-carboxylic acid

Hydroxamic acids are present in a several pharmaceuticals and agrochemicals. Synthetic strategies providing access to hydroxamic acid derivatives remain limited, typically requiring the use of nucleophilic hydroxylamine reagents. Herein, a synthesis of hydroxamates from unactivated carboxylic acids is reported making use of rare blocked (masked) O-substituted isocyanates. The applicability of this transformation was highlighted by targeting the synthesis of vorinostat and belinostat derivatives.

Safety of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Derasp, JS; Barbera, EA; Seguin, NR; Brzezinski, DD; Beauchemin, AM or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem