Month: December 2021

Recently I am researching about CARFILZOMIB; DESIGN, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21877061]; Natural Science Foundation of Jiangsu ProvinceNatural Science Foundation of Jiangsu Province [BK20171448]; National and Local Joint Engineering Research Center of Biomedical Functional Materials. Formula: C5H4N2O2. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Lei, M; Zhang, HY; Miao, H; Du, X; Zhou, H; Wang, J; Wang, XY; Feng, HY; Shi, JM; Liu, ZG; Shen, J; Zhu, YQ. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

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.

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.. Formula: C5H4N2O2

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

Recently I am researching about PHASE-II TRIAL; ORGANIC SULFUR CHEMISTRY; QUINOXALINE ANTIBIOTICS; TRIOSTIN; HYPOXIA; DESULFURIZATION; DEPSIPEPTIDES; QUINOMYCIN; PATHWAY, Saw an article supported by the JSPSMinistry of Education, Culture, Sports, Science and Technology, Japan (MEXT)Japan Society for the Promotion of Science [16H05097, 19H03345, 18H04599, 20H04757]; Hokkaido University, Global Facility Center (GFC), Pharma Science Open Unit (PSOU) – MEXT under Support Program for Implementation of New Equipment Sharing System, Platform Project for Supporting Drug Discovery and Life Science Research (Basis for Suppor [18am0101093j0002]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Kojima, K; Yakushiji, F; Katsuyama, A; Ichikawa, S. 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

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.

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.. Product Details of 98-97-5

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

Sun, Q; Zhou, TL; Xi, DD; Li, XN; Lu, ZR; Xu, FR; Wang, C; Niu, Y; Xu, P in [Sun, Qi; Zhou, Tongliang; Xi, Dandan; Li, Xiaona; Lu, Zirui; Xu, Fengrong; Wang, Chao; Niu, Yan; Xu, Ping] Peking Univ, Sch Pharmaceut Sci, Dept Med Chem, Hlth Sci Ctr, Beijing 100191, Peoples R China; [Sun, Qi] Peking Univ, Coll Chem & Mol Engn, State Key Lab Struct Chem Unstable & Stable Speci, BNLMS, Beijing 100871, Peoples R China published Design and synthesis of tripeptidyl furylketones as selective inhibitors against the beta 5 subunit of human 20S proteasome in 2020, Cited 31. 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 series of tripeptidic proteasome inhibitors with furylketone as C-terminus were designed and synthesized. Biochemical evaluations against beta 1, beta 2 and beta 5 subunits revealed that they acted selectively on beta 5 subunit with IC(50)s against chymotrypsin-like (CT-L) activity in micromolar range. LC-MS/MS analysis of the ligand-20S proteasome mixture showed that the most potent compound 11m (IC50 = 0.18 mu M) made no covalent modification on 20S proteasome. However, it was identified acting in a slowly reversible manner in wash-out assay and the reversibility was much lower than that of MG132, suggesting the possibility of these tripeptidic furylketones forming reversible covalent bonds with 20S proteasome. Several compounds were selected for anti-proliferative assay towards multiple cancer cell lines, and compound 11m displayed comparable potency to positive control (MG132) in all cell lines tested. Furthermore, the pharmacokinetic (PK) data in rats indicated 11m behaved similarly (C-max, 2007 mu g/L; AUC(0-t), 680 mu g/L.h; V-ss, 0.66 L/kg) to the clinical used agent carfilzomib. All these data suggest 11m is a good lead compound to be developed to novel anti-tumor agent. (c) 2020 Elsevier Masson SAS. All rights reserved.

Welcome to talk about 98-97-5, If you have any questions, you can contact Sun, Q; Zhou, TL; Xi, DD; Li, XN; Lu, ZR; Xu, FR; Wang, C; Niu, Y; Xu, P or send Email.. SDS of cas: 98-97-5

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

Liu, J; Zhang, GY; Zhang, Z; Li, B; Chai, F; Wang, Q; Zhou, ZD; Xu, LL; Wang, SK; Jin, Z; Tang, YZ in [Liu, Jie; Zhang, Guang-Yu; Zhang, Zhe; Li, Bo; Chai, Fei; Wang, Qi; Zhou, Zi-Dan; Xu, Ling-Ling; Wang, Shou-Kai; Jin, Zhen; Tang, You-Zhi] South China Agr Univ, Coll Vet Med, Guangdong Prov Key Lab Vet Pharmaceut Dev & Safet, Guangzhou 510642, Peoples R China; [Jin, Zhen; Tang, You-Zhi] Guangdong Lab Lingnan Modern Agr, Guangzhou 510642, Peoples R China published Design, synthesis, in vitro and in vivo evaluation against MRSA and molecular docking studies of novel pleuromutilin derivatives bearing 1, 3, 4-oxadiazole linker in 2021, Cited 29. Recommanded Product: 98-97-5. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A class of pleuromutilin derivatives containing 1, 3, 4-oxadiazole were designed and synthesized as potential antibacterial agents against Methicillin-resistant staphylococcus aureus (MRSA). The ultrasound-assisted reaction was proposed as a green chemistry method to synthesize 1, 3, 4-oxadiazole derivatives (intermediates 85-110). Among these pleuromutilin derivatives, compound 133 was found to be the strongest antibacterial derivative against MRSA (MIC = 0.125 mu g/mL). Furthermore, the result of the time-kill curves displayed that compound 133 could inhibit the growth of MRSA in vitro quickly (- 4.36 log10 CFU/mL reduction). Then, compound 133 (1.82 log10 CFU/mL) displayed superior in vivo antibacterial efficacy than tiamulin (- 0.82 log10 CFU/mL) in reducing MRSA load in mice thigh model. Besides, compound 133 exhibited low cytotoxicity to RAW 264.7 cells. Molecular docking studies revealed that compound 133 was successfully localized in the binding pocket of 50S ribosomal subunit (delta Gb = -10.50 kcal/mol). The results indicated that these pleuromutilin derivatives containing 1, 3, 4-oxadiazole might be further developed into novel antibiotics against MRSA.

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.. Recommanded Product: 98-97-5

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

Formula: C5H4N2O2. In 2019 CHEMISTRYSELECT published article about PI-PI STACKING; UNCONVENTIONAL HYDROGEN-BONDS; DOT-HC INTERACTIONS; COORDINATION POLYMERS; ELECTRON-DENSITY; HALOGEN BOND; MOLECULAR TECTONICS; CRYSTAL-STRUCTURE; QUANTUM-THEORY; CHEMICAL-BOND in [Khavasi, Hamid Reza; Balmohammadi, Yaser] Shahid Beheshti Univ, Dept Inorgan Chem & Catalysis, Gen Campus, Tehran 1983963113, Iran; [Naghavi, S. Shahab] Shahid Beheshti Univ, GC, Dept Phys & Computat Chem, Tehran 1983963113, Iran in 2019, Cited 97. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

The nature of the attractive intermolecular C-H horizontal ellipsis H-C interaction, which could affect the crystal packing and solid-state molecular structure, is yet unknown. Here, a novel mercury (II) complex including N-(2-biphenyl)pyrazine-2-carboxamide ligand, one such system, has been synthesized and characterized by a single crystal X-ray diffraction. The existence of attractive intermolecular C-HMIDLINE HORIZONTAL ELLIPSISH-C interaction (-2.64 to -9.30 kj/mol depending on computational levels) is a notable feature in the crystal packing of this complex, which is the first observation of intermolecular C-HMIDLINE HORIZONTAL ELLIPSISH-C interaction in a metal complex. From crystallographic data, this contact has a distance of 2.172 angstrom which is 9.5% shorter than the sum of the van der Waals radii of two hydrogen atoms, which is the primary condition of having intermolecular interactions. We study the nature C-H horizontal ellipsis H-C interaction in the synthesized mercury (II) complex using periodic/non-periodic density functional theory in conjunction with quantum theory of atoms in molecules, non-covalent interaction reduced density gradient method, natural bond orbital, and energy decomposition analysis tools. Our results suggest that C-HMIDLINE HORIZONTAL ELLIPSISH-C interaction has closed-shell, donor-acceptor, and van der Waals nature.

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.. Formula: C5H4N2O2

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

Authors Zhao, HY; Wang, B; Fu, L; Li, G; Lu, HJ; Liu, YK; Sheng, L; Li, Y; Zhang, BX; Lu, Y; Ma, C; Huang, HH; Zhang, DF; Lu, Y in AMER CHEMICAL SOC published article about BENZOXAZINYL-OXAZOLIDINONES; MYCOBACTERIUM-TUBERCULOSIS; BACTERICIDAL ACTIVITY; IN-VITRO; POTENT; ANALOGS; DESIGN in [Zhao, Hongyi; Li, Gang; Lu, Haijia; Huang, Haihong; Zhang, Dongfeng] Chinese Acad Med Sci & Peking Union Med Coll, Chinese Acad Med Sci, Beijing Key Lab Act Subst Discovery & Druggabil E, Key Lab AntiDR TB Innovat Drug Res,Inst Mat Med, Beijing 100050, Peoples R China; [Wang, Bin; Fu, Lei; Lu, Yu] Capital Med Univ, Beijing Chest Hosp, Beijing TB & Thorac Tumor Res Inst, Beijing Key Lab Drug Resistance TB Res,Dept Pharm, Beijing 101149, Peoples R China; [Liu, Yuke; Sheng, Li; Li, Yan] Chinese Acad Med Sci & Peking Union Med Coll, Chinese Acad Med Sci, Beijing Key Lab Nonclin Drug Metab & PK PD Study, Key Lab AntiDR TB Innovat Drug Res,Inst Mat Med, Beijing 100050, Peoples R China; [Zhang, Baoxi; Lu, Yang] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China; [Ma, Chen] Chinese Acad Med Sci & Peking Union Med Coll, Chinese Acad Med Sci, Beijing Key Lab Polymorph Drugs, Key Lab AntiDR TB Innovat Drug Res,Inst Mat Med, Beijing 100050, Peoples R China in 2020, Cited 30. 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

Tuberculosis (TB) remains a serious public health challenge, and the research and development of new anti-TB drugs is an essential component of the global strategy to eradicate TB. In this work, we discovered a conformationally constrained oxazolidinone 19c with improved anti-TB activity and safety profile through a focused lead optimization effort. Compound 19c displayed superior in vivo efficacy in a mouse TB infection model compared to linezolid and sutezolid. The druggability of compound 19c was demonstrated in a panel of assays including microsomal stability, cytotoxicity, cytochrome P450 enzyme inhibition, and pharmacokinetics in animals. Compound 19c demonstrated an excellent safety profile in a battery of safety assays, including mitochondrial protein synthesis, hERG K+, hCav1.2, and Nav1.5 channels, monoamine oxidase, and genotoxicity. In a 4 week repeated dose toxicology study in rats, 19c appeared to have less bone marrow suppression than linezolid, which has been a major liability of the oxazolidinone class.

Product Details of 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Zhao, HY; Wang, B; Fu, L; Li, G; Lu, HJ; Liu, YK; Sheng, L; Li, Y; Zhang, BX; Lu, Y; Ma, C; Huang, HH; Zhang, DF; Lu, Y or send Email.

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

An article Molecular design aided by random forests and synthesis of potent trypanocidal agents as cruzain inhibitors for Chagas disease treatment WOS:000577619900006 published article about CYSTEINE PROTEASE; TRYPANOSOMA-CRUZI; DRUG DISCOVERY; INTEGRATION; ISOFORMS; LIGANDS; IMPROVE in [de Albuquerque, Sergio; Duque, Carla; da Silva, Joao Santana] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Sao Paulo, Brazil; [Cianni, Lorenzo; de Vita, Daniela; Leitao, Andrei; Montanari, Carlos A.; Ribeiro, Jean F. R.] Univ Sao Paulo, Inst Quim Sao Carlos, Grp Quim Med, Ave Trabalhador Sancarlense 400, BR-13566590 Sao Carlos, SP, Brazil; [Gomes, Ana S. M.; Gomes, Paula; Teixeira, Catia] Univ Porto, Dept Quim & Bioquim, LAQV REQUIMTE, Fac Ciencias, Porto, Portugal; [Laughton, Charles] Univ Nottingham, Sch Pharm, Nottingham, England; [Laughton, Charles] Univ Nottingham, Ctr Biomol Sci, Nottingham, England; [Montanari, Raphael] Univ Sao Paulo, Ctr Robot Sao Carlos, EESC ICMC, Sao Paulo, Brazil; [Ribeiro, Jean F. R.] Univ Fed Goias, Inst Trop Pathol & Publ Hlth, Goiania, Go, Brazil in 2020, Cited 59. Application In Synthesis of Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Cruzain is an established target for the identification of novel trypanocidal agents, but how good are in vitro/in vivo correlations? This work describes the development of a random forests model for the prediction of the bioavailability of cruzain inhibitors that areTrypanosoma cruzikillers. Some common properties that characterize drug-likeness are poorly represented in many established cruzain inhibitors. This correlates with the evidence that many high-affinity cruzain inhibitors are not trypanocidal agents againstT. cruzi. On the other hand,T. cruzikillers that present typical drug-like characteristics are likely to show better trypanocidal action than those without such features. The random forests model was not outperformed by other machine learning methods (such as artificial neural networks and support vector machines), and it was validated with the synthesis of two new trypanocidal agents. Specifically, we report a new lead compound,Neq0565, which was tested onT. cruziTulahuen (beta-galactosidase) with a pEC(50)of 4.9. It is inactive in the host cell line showing a selectivity index (SI = EC50cyto/EC50T. cruzi) higher than 50.

Welcome to talk about 98-97-5, If you have any questions, you can contact de Albuquerque, S; Cianni, L; de Vita, D; Duque, C; Gomes, ASM; Gomes, P; Laughton, C; Leitao, A; Montanari, CA; Montanari, R; Ribeiro, JFR; da Silva, JS; Teixeira, C or send Email.. Application In Synthesis of Pyrazine-2-carboxylic acid

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

Authors Samie, A; Salimi, A; Garrison, JC in ROYAL SOC CHEMISTRY published article about INDEPENDENT CHEMICAL-SHIFTS; THROUGH-SPACE INTERACTIONS; FACE-TO-FACE; HYDROGEN-BOND; CRYSTAL-STRUCTURE; CURRENT-DENSITY; SANDWICH; SUBSTITUENTS; COMPLEXES; ENERGIES in [Samie, Ali; Salimi, Alireza] Ferdowsi Univ Mashhad, Fac Sci, Dept Chem, Mashhad, Iran; [Garrison, Jered C.] Univ Nebraska Med Ctr, Dept Pharmaceut Sci, Omaha, NE USA in 2019, Cited 72. Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Based on the crystal engineering concept, four new esters containing alpha and beta-substituted naphthalene rings were designed, synthesized and fully characterized. The crystal structure analysis of the designed molecules revealed that the C-H-based interactions especially C-HMIDLINE HORIZONTAL ELLIPSIS pi have a significant role in the stabilization of crystal architectures. Regarding the molecular structure of naphthalene rings, one can find that bond lengths are divided into two groups (shorter and longer) so that relative localization is likely to occur in this system. Since pi-electron localization in aromatic rings has been previously introduced as responsible for stronger pi-stacking, this issue was investigated through C-HMIDLINE HORIZONTAL ELLIPSIS pi interaction in this study. Cambridge Structural Database (CSD) analysis was performed by exploration of suitable geometries for C-HMIDLINE HORIZONTAL ELLIPSIS pi(c) and C-HMIDLINE HORIZONTAL ELLIPSIS pi(e) in naphthalene and phenol systems (pi(c) and pi(e) are the centre and edge of the aromatic rings, respectively). The tendency factor (TF) of the C-H moiety toward ring bonds as a new CSD-based criterion was used to detect some of the resonance forms in aromatic rings. The results indicated that C-HMIDLINE HORIZONTAL ELLIPSIS pi(e) is a ubiquitous interaction which can be employed as an experimental probe for the detection of pi-localization in naphthalene rings. Systematic experimental studies, structural evidence and computational results on the title compounds confirmed the relative pi-electron localization, as well.

Formula: C5H4N2O2. 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

Authors Huang, YZ; Zhang, Y; Li, JM; Ma, XD; Hu, MQ; Yang, Y; Gao, SF in LIPPINCOTT WILLIAMS & WILKINS published article about INHIBITORS; DISCOVERY; POTENT; ANGIOGENESIS; SAR in [Huang, Yuanzheng; Zhang, Yang; Li, Jiaming; Ma, Xiaodong; Hu, Mengqi; Yang, Yu; Gao, Sufan] Anhui Acad Chinese Med, Sch Pharm, Dept Pharmaceut Chem, Hefei, Anhui, Peoples R China; [Li, Jiaming; Ma, Xiaodong] Anhui Acad Chinese Med, Dept Med Chem, Hefei, Anhui, Peoples R China in 2019, Cited 18. Quality Control of Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

A novel structural series of tetrahydroisoquinoline-based compounds that incorporate the diaryl urea moiety was designed, synthesized, and biologically evaluated as suppressors of VEFGR-2 signaling. As a consequence, compounds 9k and 9s exhibited comparable or superior cytotoxic activity to that of gefitinib against the tested three cell lines, including A549, MCF-7, and PC-3. Importantly, both of them downregulated the expression of VEGFR-2, and inhibited VEGFR-2 phosphorylation at the concentration of 0.5 or 1.0 mu mol/ l. Besides, they suppressed human umbilical vein endothelial cell tube formation at the concentration of 4.0 mu mol/ l. Considering their capability of down-regulating VEGFR-2 expression and inhibiting VEGFR-2 phosphorylation, 9k and 9s may serve as suppressors of angiogenesis for further investigation. Copyright (c) 2018 Wolters Kluwer Health, Inc. All rights reserved.

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.. Quality Control of Pyrazine-2-carboxylic acid

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

Authors Yang, YJ; Wang, K; Yang, Y; Lai, FF; Chen, XG; Xiao, ZY in TAYLOR & FRANCIS LTD published article about in [Yang, Ya-Jun; Wang, Ke; Yang, Ying; Xiao, Zhi-Yan] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, Beijing Key Lab Active Subst Discovery & Druggabi, Beijing 100050, Peoples R China; [Lai, Fang-Fang; Chen, Xiao-Guang] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China in 2021, Cited 21. 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

Based on the interaction modes of the natural 20S proteasome inhibitors TMC-95A, we have previously discovered a dipeptide 1. To explore the SAR around compound 1, we designed and synthesized a series of dipeptides (8-38) with a fragment-based strategy. Among them, nine compounds showed significant inhibitory activities against the chymotrypsin-like activity of human 20S proteasome with IC50 values at the submicromolar level, which were comparable or even superior to the parent compound 1. Meanwhile, they displayed no significant inhibition against trypsin-like and caspase-like activities of 20S proteasome. The results suggested the feasibility to design dipeptides as novel and potent 20S proteasome inhibitors.

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