Month: October 2021

Recommanded Product: Pyrazine-2-carboxylic acid. Recently I am researching about 5-HYDROXYPYRAZINOIC ACID; NICOTINIC-ACID; RAT; CONSUMPTION; MECHANISM; PLASMA; URINE, Saw an article supported by the German Federal Ministry of Education and Research (BMBF)Federal Ministry of Education & Research (BMBF) [0315692]. Published in WILEY in HOBOKEN ,Authors: Kremer, JI; Pickard, S; Stadlmair, LF; Glass-Theis, A; Buckel, L; Bakuradze, T; Eisenbrand, G; Richling, E. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Scope Coffee is a complex mixture of over 1000 compounds, including diverse heteroaromatic compounds such as alkylpyrazines. Little is known about the intake, metabolism, and bodily distribution of these compounds. Therefore, a human intervention study is conducted to investigate the excretion of alkylpyrazine metabolites in urine after the ingestion of brewed coffee containing alkylpyrazines. Methods and results After consuming a diet without heat-processed food, ten volunteers consumed 500 mL of freshly brewed coffee prepared from coffee pads, providing intakes of 2-methylpyrazine (2-MeP), 2,5-dimethylpyrazine (2,5-DMeP), and 2,6-dimethylpyrazine (2,6-DMeP) amounting to 17.2, 4.4, and 4.9 mu mol, respectively. These alkylpyrazines are metabolized into the corresponding pyrazine carboxylic acids, namely pyrazine-2-carboxylic acid (PA), 5-hydroxypyrazine-2-carboxylic acid (5-OHPA), 5-methylpyrazine-2-carboxylic acid (5-MePA), and 6-methylpyrazine-2-carboxylic acid (6-MePA). In total, 64% of the ingested 2-MeP is excreted as PA, as well as 26% as 5-OHPA, while 91% and 97% of the ingested 2,5-DMeP and 2,6-DMeP are recovered as 5-MePA and 6-MePA, respectively, in urine samples collected after coffee consumption. Conclusion This study provides evidence that alkylpyrazines are rapidly metabolized into the corresponding carboxylic acids and excreted via urine by humans, which is consistent with earlier rodent studies.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Kremer, JI; Pickard, S; Stadlmair, LF; Glass-Theis, A; Buckel, L; Bakuradze, T; Eisenbrand, G; Richling, E or concate me.. Recommanded Product: Pyrazine-2-carboxylic acid

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

An article A novel hydrazide Schiff base self-assembled nanoprobe for selective detection of human serum albumin and its applications in renal disease surveillance WOS:000572109900016 published article about SENSITIVE FLUORESCENT-PROBE; HSA; SENSOR; RECOGNITION; SITE; QUANTIFICATION; FLUOROPHORES; DIAGNOSIS; INSIGHTS; BINDING in [Wang, Zhi-Gang; Yan, Xiao-Jing; Xie, Cheng-Zhi; Xu, Jing-Yuan] Tianjin Med Univ, Sch Pharm, Dept Chem Biol, Tianjin 300070, Peoples R China; [Wang, Zhi-Gang; Yan, Xiao-Jing; Xie, Cheng-Zhi; Xu, Jing-Yuan] Tianjin Med Univ, Sch Pharm, Tianjin Key Lab Technol Enabling Dev Clin Therape, Tianjin 300070, Peoples R China; [Liu, Hai-Bo] Chinese Acad Med Sci, Peking Union Med Coll, Inst Med Plant Dev, Beijing 100193, Peoples R China; [Zhang, De-Long] Tianjin Santan Hosp, Dept Pharm, Tianjin 300193, Peoples R China; [Liu, Wei] Tianjin Med Univ, Hosp 2, Tianjin 300211, Peoples R China; [Li, Qing-Zhong] Yantai Univ, Sch Chem & Chem Engn, Lab Theoret & Computat Chem, Yantai 264005, Peoples R China in 2020, Cited 53. Recommanded Product: Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Human serum albumin (HSA) is considered as a biomarker for the early diagnosis of renal disease, therefore identifying and detecting HSA in biological fluids (especially urine) with an easy method is of great importance. Herein, we report a novel hydrazide Schiff base fluorescent probeN ‘-((7-(diethylamino)-2-oxo-2H-chromen-3-yl)methylene)pyrazine-2-carbohydrazide (NPC), which self-assembled into nanoparticles in aqueous solution. Based on disassembly-induced emission and the site-specific recognition mechanism, the binding ofNPCwith HSA resulted in a fluorescence turn-on response. ProbeNPCexhibited superior selectivity and sensitivity toward HSA with a detection limit of 0.59 mg L(-1)in PBS and 0.56 mg L(-1)in the urine sample. The site-binding mechanism ofNPCwith HSA was explored by fluorescence quenching study, Job’s plot analysis, HSA destruction, site marker displacement and molecular docking. Fluorescence imaging of HSA in MCF-7 cells was achieved by using a non-toxicNPCprobe, suggesting thatNPCcould be applied to visualize the level of HSAin vivo. More importantly, further practical applications of probeNPCin human urine samples were achieved with satisfactory results by using a fluorometer or test paper, which could provide extensive application in clinical diagnosis.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Wang, ZG; Yan, XJ; Liu, HB; Zhang, DL; Liu, W; Xie, CZ; Li, QZ; Xu, JY or concate me.. Recommanded Product: Pyrazine-2-carboxylic acid

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

Recommanded Product: 98-97-5. Authors Guin, S; Dolui, P; Zhang, XL; Paul, S; Singh, VK; Pradhan, S; Chandrashekar, HB; Anjana, SS; Paton, RS; Maiti, D in WILEY-V C H VERLAG GMBH published article about in [Guin, Srimanta; Dolui, Pravas; Paul, Satyadip; Singh, Vikas Kumar; Pradhan, Sukumar; Chandrashekar, Hediyala B.; Anjana, S. S.; Maiti, Debabrata] Indian Inst Technol, Dept Chem, Mumbai 400076, Maharashtra, India; [Zhang, Xinglong; Paton, Robert S.] Univ Oxford, Chem Res Lab, Dept Chem, Mansfield Rd, Oxford OX1 3TA, England in 2019, Cited 72. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Directed C-H functionalization has been realized as a complementary tool to the traditional approaches for a straightforward access of non-proteinogenic amino acids; albeit such a process is restricted mostly up to the gamma-position. In the present work, we demonstrate the diverse (hetero) arylation of amino acids and analogous aliphatic amines selectively at the remote delta-position by tuning the reactivity controlled by ligands. An organopalladium delta-C(sp(3))-H activated intermediate has been isolated and crystallographically characterized. Mechanistic investigations carried out experimentally in conjunction with computational studies shed light on the difference in the mechanistic picture depending on the substrate structure.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Guin, S; Dolui, P; Zhang, XL; Paul, S; Singh, VK; Pradhan, S; Chandrashekar, HB; Anjana, SS; Paton, RS; Maiti, D or concate me.. Recommanded Product: 98-97-5

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

An article Design, synthesis, and biological evaluation of tetrahydroisoquinoline-based diaryl urea derivatives for suppressing VEGFR-2 signaling WOS:000466009600010 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. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Quality Control of Pyrazine-2-carboxylic acid

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.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Huang, YZ; Zhang, Y; Li, JM; Ma, XD; Hu, MQ; Yang, Y; Gao, SF or concate me.. Quality Control of Pyrazine-2-carboxylic acid

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

An article N-(4-(2-chloro-4-(trifluoromethyl)phenoxy)phenyl)picolinamide as a new inhibitor of mitochondrial complex III: Synthesis, biological evaluation and computational simulations WOS:000546629300011 published article about CYTOCHROME BC(1) COMPLEX; IRON-SULFUR PROTEIN; BC1 COMPLEX; DISCOVERY; SITE; FUNGICIDE; AMETOCTRADIN; RESISTANCE; MECHANISM; BINDING in [Cheng, Hua; Yang, Lu; Liu, Hong-Fu; Zhang, Rui] Hubei Univ Arts & Sci, Dept Chem Engn & Food Sci, Xiangyang 441053, Peoples R China; [Chen, Cheng] Wuhan Univ Technol, State Key Lab Adv Technol Mat Synth & Proc, Wuhan 430070, Peoples R China; [Wu, Yuan; Jiang, Wen] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China in 2020, Cited 47. HPLC of Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Mitochondrial complex III is one of the most promising targets for a number of pharmaceuticals and fungicides. Due to the wide-spread use of complex III-inhibiting fungicides, a considerable increase of resistance has occurred worldwide. Therefore, inhibitors with novel scaffolds and potent activity against complex III are still in great demand. In this article, a new series of amide compounds bearing the diaryl ether scaffold were designed and prepared, followed by the biological evaluation. Gratifyingly, several compounds demonstrated potent activity against succinate-cytochrome c reductase (SCR, a mixture of mitochondrial complex II and complex III), with compound 3w possessing the best inhibitory activity (IC50 = 0.91 +/- 0.09 mu mol/L). Additional studies verified that 3w was a new inhibitor of complex III. Moreover, computational simulations elucidated that 3w should bind to the Q(o) site of complex III. We believe this work will be valuable for the preparation and discovery of more complex III inhibitors.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Cheng, H; Yang, L; Liu, HF; Zhang, R; Chen, C; Wu, Y; Jiang, W or concate me.. HPLC of Formula: C5H4N2O2

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

In 2020 EUR J MED CHEM published article about NONCOVALENT; APOPTOSIS; PATHWAY; POTENT 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 in 2020, Cited 31. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Application In Synthesis of Pyrazine-2-carboxylic acid

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.

About Pyrazine-2-carboxylic acid, 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 concate me.. Application In Synthesis of Pyrazine-2-carboxylic acid

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

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers in Vitro and in Vivo published in 2020. Recommanded Product: 98-97-5, Reprint Addresses Bao, R; Luo, YF (corresponding author), Sichuan Univ, State Key Lab Biotherapy, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China.; Bao, R; Luo, YF (corresponding author), Sichuan Univ, Canc Ctr, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Caseinolytic protease P (ClpP) is considered as a promising target for the treatment of Staphylococcus aureus infections. In an unbiased screen of 2632 molecules, a peptidomimetic boronate, MLN9708, was found to be a potent suppressor of SaClpP function. A time-saving and cost-efficient strategy integrating in silico position scanning, multistep miniaturized synthesis, and bioactivity testing was deployed for optimization of this hit compound and led to fast exploration of structure-activity relationships. Five of 150 compounds from the miniaturized synthesis exhibited improved inhibitory activity. Compound 43Hf was the most active inhibitor and showed reversible covalent binding to SaClpP while did not destabilize the tetradecameric structure of SaClpP. The crystal structure of 43Hf-SaClpP complex provided mechanistic insight into the covalent binding mode of peptidomimetic boronate and SaClpP. Furthermore, 43Hf could bind endogenous ClpP in S. aureus cells and exhibited significant efficacy in attenuating S. aureus virulence in vitro and in vivo.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Ju, Y; He, LH; Zhou, YZ; Yang, T; Sun, K; Song, R; Yang, Y; Li, CW; Sang, ZT; Bao, R; Luo, YF or concate me.. Recommanded Product: 98-97-5

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

I found the field of Biochemistry & Molecular Biology; Pharmacology & Pharmacy very interesting. Saw the article Discovery ofN-(1-(3-fluorobenzoyl)-1H-indol-5-yl)pyrazine-2-carboxamide: a novel, selective, and competitive indole-based lead inhibitor for human monoamine oxidase B published in 2020. Computed Properties of C5H4N2O2, Reprint Addresses Elkamhawy, A (corresponding author), Dongguk Univ Seoul, Coll Pharm, Goyang 10326, South Korea.; Roh, EJ (corresponding author), Korea Inst Sci & Technol KIST, Chem Kin Res Ctr, Seoul 02792, South Korea.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Herein, two new series ofN-substituted indole-based analogues were rationally designed, synthesizedviamicrowave heating technology, and evaluated as noteworthy MAO-B potential inhibitors. Compared to the reported indazole-based hitsVIandVII, compounds4band4eexhibited higher inhibitory activities over MAO-B with IC(50)values of 1.65 and 0.78 mu M, respectively. When compared to the modest selectivity index of rasagiline (II, a well-known MAO-B inhibitor, SI > 50), both4band4ealso showed better selectivity indices (SI > 60 and 120, respectively). A further kinetic evaluation of the most potent derivative (4e) displayed a competitive mode of inhibition (inhibition constant (K-i)/MAO-B = 94.52 nM). Reasonable explanations of the elicited biological activities were presentedviaSAR study and molecular docking simulation. Accordingly, the remarkable MAO-B inhibitory activity of4e(N-(1-(3-fluorobenzoyl)-1H-indol-5-yl)pyrazine-2-carboxamide), with its selectivity and competitive inhibition, advocates its potential role as a promising lead worthy of further optimization.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Elkamhawy, A; Paik, S; Kim, HJ; Park, JH; Londhe, AM; Lee, K; Pae, AN; Park, KD; Roh, EJ or concate me.. Computed Properties of C5H4N2O2

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

In 2020 BIOORG MED CHEM LETT published article about PHARMACOLOGICAL EVALUATION; ANTIBACTERIAL ACTIVITY; ANTIMICROBIAL ACTIVITY; ACCURATE DOCKING; OXAZOLIDINONE; OXADIAZOLES; DESIGN; GLIDE in [Kashid, Bharat B.; Salunkhe, Pravin H.; Dongare, Balasaheb B.; Ghanwat, Anil A.] Solapur Univ, Sch Chem Sci, Chem Res Lab, Solapur 413255, India; [Salunkhe, Pravin H.] CSIR Natl Chem Lab, Dr Homi Bhabha Rd, Pune 411008, Maharashtra, India; [More, Kishor R.] Shandong Keyuan Pharmaceut Co Ltd, Keyuan St, Jinan, Shandong, Peoples R China; [Khedkar, Vijay M.] Vishwakarma Univ, Sch Pharm, Survey 2,3,4 Laxminagar, Pune 411048, Maharashtra, India in 2020, Cited 43. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. COA of Formula: C5H4N2O2

A series of novel 2, 5-disubstituted 1, 3, 4-Oxadiazole derivatives as a potential anti-inflammatory, and antioxidant agent were synthesized via cyclisation. Hydrazide molecule treated with substituted acids in the presence of phosphorus oxychloride (POCl3) as an efficient reagent as well as solvent by conventional method with shorter reaction time and excellent yield. The newly synthesized 1, 3, 4-oxadiazole derivatives exhibited excellent to good anti-inflammatory and anti-oxidant activities compaired to the standard drugs. Molecular docking study on the crucial anti-inflammatory target-cyclooxygenase-2 (COX-2) revealed the ability of the scaffold to correctly recognize the active site and achieve significant bonded and non-bonded interactions with key residues therein. This study could identify potential compounds which can be pertinent starting points for structure-based drug design to obtain newer anti-inflammatory agents.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Kashid, BB; Salunkhe, PH; Dongare, BB; More, KR; Khedkar, VM; Ghanwat, AA or concate me.. COA of Formula: C5H4N2O2

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

An article Synthesis, antimicrobial and chitinase inhibitory activities of 3-amidocoumarins WOS:000526784800049 published article about ANTIFUNGAL; CONDENSATION; ALLOSAMIDIN; DERIVATIVES; RESISTANCE; COUMARINS; SCAFFOLD; ARGADIN; AGENTS in [Sharma, Rajesh Kumar; Tiwari, Neha; Katiyar, Diksha] Banaras Hindu Univ, Dept Chem, MMV, Varanasi 221005, Uttar Pradesh, India; [Singh, Vineeta] Inst Engn & Technol, Dept Biotechnol, Sitapur Rd, Lucknow 226021, Uttar Pradesh, India; [Butcher, R. J.] Howard Univ, Dept Chem, 525 Coll St NW, Washington, DC 20059 USA in 2020, Cited 45. 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

A series of 3-amidocoumarins has been synthesized and tested in vitro for their anitimicrobial and chitinase inhibitory activities. Among these, compounds 5k, 5l, 8b-8d, 8f and 8g exhibited good antibacterial activity with MIC values in the range of 6.25-25 mu g/mL against some of the tested strains while compounds 5l, 8b, 8c and 8f showed good activity against at least one or two fungal strains. Some of the assayed compounds 5d, 5k, 5l, 8b and 8c displayed significant chitinase inhibitory activity with IC50, values in the range of 3.74-5.6 mu M. Among them, 5l proved to be potent chitinase inhibitor with IC50 value of 3.74 mu M. To better understand the enzyme-inhibitor interactions molecular docking study of all the synthesized compounds was carried out on Aspergillus fumigatus chitinase 1W9U. The compound 5l showed high binding affinity with the receptor with binding energy value of -8.44 Kcal/mol. This study also provides structure activity relationship (SAR) of synthesized compounds.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Sharma, RK; Singh, V; Tiwari, N; Butcher, RJ; Katiyar, D or concate me.. Application In Synthesis of Pyrazine-2-carboxylic acid

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