Month: November 2021

Recommanded Product: 98-97-5. In 2020 NAT COMMUN published article about ASPARTATE DECARBOXYLASE; SUSCEPTIBILITY; PANTOTHENATE; MUTATIONS; MODEL in [Sun, Qingan; Li, Xiaojun; Sacchettini, James C.] Texas A&M Univ, Dept Biochem & Biophys, College Stn, TX 77843 USA; [Perez, Lisa M.] Texas A&M Univ, Lab Mol Simulat, College Stn, TX USA; [Shi, Wanliang; Zhang, Ying] Johns Hopkins Univ, Bloomberg Sch Publ Hlth, Dept Mol Microbiol & Immunol, Baltimore, MD 21205 USA in 2020, Cited 30. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Pyrazinamide has been a mainstay in the multidrug regimens used to treat tuberculosis. It is active against the persistent, non-replicating mycobacteria responsible for the protracted therapy required to cure tuberculosis. Pyrazinamide is a pro-drug that is converted into pyrazinoic acid (POA) by pyrazinamidase, however, the exact target of the drug has been difficult to determine. Here we show the enzyme PanD binds POA in its active site in a manner consistent with competitive inhibition. The active site is not directly accessible to the inhibitor, suggesting the protein must undergo a conformational change to bind the inhibitor. This is consistent with the slow binding kinetics we determined for POA. Drug-resistant mutations cluster near loops that lay on top of the active site. These resistant mutants show reduced affinity and residence time of POA consistent with a model where resistance occurs by destabilizing the closed conformation of the active site. The important tuberculosis drug pyrazinamide (PZA) is converted to its active form pyrazinoic acid (POA) in Mycobacterium tuberculosis (Mtb). Here the authors identify the pantothenate biosynthesis pathway enzyme aspartate decarboxylase (PanD) as the target of PZA and determine the POA bound Mtb PanD crystal structure.

Recommanded Product: 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Sun, QG; Li, XJ; Perez, LM; Shi, WL; Zhang, Y; Sacchettini, JC or send Email.

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

Computed Properties of C5H4N2O2. Authors Packiaraj, S; Kousalya, L; Pushpaveni, A; Poornima, S; Puschmann, H; Govindarajan, S in SPRINGER published article about in [Packiaraj, S.] Sri Krishna Coll Engn & Technol, Sci & Humanities Chem, Coimbatore 641008, Tamil Nadu, India; [Packiaraj, S.; Pushpaveni, A.; Poornima, S.; Govindarajan, S.] Bharathiar Univ, Dept Chem, Coimbatore 641046, Tamil Nadu, India; [Kousalya, L.] Nirmala Coll Women, Dept Bot, Coimbatore 641018, Tamil Nadu, India; [Pushpaveni, A.] Kongunadu Arts & Sci Coll, Dept Chem, Coimbatore 641029, Tamil Nadu, India; [Puschmann, H.] Univ Durham, Dept Chem, South Rd, Durham DH1 3LE, England in 2021, Cited 43. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

In general, molecules with certain functional groups such as amine (-NH2) and carboxyl (-COOH) can promote the growth of co-crystals leading to the formation of supramolecular networks. However, if the differences in the pKa values of the two molecules are large [pKa (base)-pKa (acid)], salts can result instead of ‘real’ co-crystals. Here, we report the formation of such salt by letting pyrazine-2-carboxylic acid (pKa = 2.9) crystallize together with aminoguanidine (pKa = 11.5; high Delta pka = 8.6) a nitrogen-rich organic base. The title salt has been prepared by slow evaporation of an equimolar ratio of guanylhydrazine bicarbonate (i.e., aminoguanidine bicarbonate (AgunH.HCO3)) and pyrazine-2-carboxylic acid (Pymca) in aqueous medium. The salt was characterized by IR spectroscopy, powder and single-crystal X-ray diffraction techniques. This material shows enhanced antioxidant activity and this is due to the crucial role of hydrazinic moiety in the aminoguanidinium salt.

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.. Computed Properties of C5H4N2O2

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

An article Novel Homo-Bivalent and Polyvalent Compounds Based on Ligustrazine and Heterocyclic Ring as Anticancer Agents WOS:000507299600083 published article about SIGNALING PATHWAY; NATURAL-PRODUCTS; DERIVATIVES; APOPTOSIS; DESIGN; DISCOVERY; PREDICTION; CURCUMIN; ACID in [Wang, Jiawen; Liu, Tianjun] Tianjin Univ Tradit Chinese Med, Grad Inst, Tianjin 301617, Peoples R China; [Hong, Ge; Li, Guoliang; Wang, Wenzhi; Liu, Tianjun] Chinese Acad Med Sci & Peking Union Med Coll, Inst Biomed Engn, Tianjin Key Lab Biomed Mat, Tianjin 300192, Peoples R China; [Hong, Ge; Liu, Tianjun] 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 2019, Cited 30. 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

Bivalent and polyvalent inhibitors can be used as antitumor agents. In this experiment, eight ligustrazine dimers and seven ligustrazine tetramers linked by alkane diamine with different lengths of carbon chain lengths were synthesized. After screening their antiproliferation activities against five cancer cell lines, most ligustrazine derivatives showed better cytotoxicity than the ligustrazine monomer. In particular, ligustrazine dimer 8e linked with decane-1,10-diamine exhibited the highest cytotoxicity in FaDu cells with an IC50 (50% inhibiting concentration) value of 1.36 nM. Further mechanism studies suggested that 8e could induce apoptosis of FaDu cells through the depolarization of mitochondrial membrane potential and S-phase cell cycle arrest. Inspired by these results, twenty-seven additional small molecule heterocyclic dimers linked with decane-1,10-diamine and nine cinnamic acid dimers bearing ether chain were synthesized and screened. Most monocyclic and bicyclic aromatic systems showed highly selective anti-proliferation activity to FaDu cells and low toxicity to normal MCF 10A cells. The structure-activity relationship revealed that the two terminal amide bonds and the alkyl linker with a chain length of 8-12 carbon were two important factors to maintain its antitumor activity. In addition, the ADMET calculation predicted that most of the potent compounds had good oral bioavailability.

Welcome to talk about 98-97-5, If you have any questions, you can contact Wang, JW; Hong, G; Li, GL; Wang, WZ; Liu, TJ or send Email.. Safety of Pyrazine-2-carboxylic acid

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

An article Synthesis of Hydroxamic Acid Derivatives Using Blocked (Masked) O-Isocyanate Precursors WOS:000574921100067 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. Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

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.

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.. Formula: C5H4N2O2

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

Computed Properties of C5H4N2O2. I found the field of Chemistry very interesting. Saw the article A chromone based Schiff base: An efficient colorimetric sensor for specific detection of Cu (II) ion in real water samples published in 2021, Reprint Addresses Malhotra, R (corresponding author), Guru Jambheshwar Univ Sci & Technol, Dept Chem, Hisar 125001, Haryana, India.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid.

A new chromone based Schiff base ligand L was synthesized by the condensation of 3-formyl chromone and pyrazine-2-carbohydrazide as a colorimetric probe to detect Cu (II) ions selectively. An instant visual colour change from colourless to yellow was obtained on addition of Cu2+ ions to the probe L solution, while other metal ions found ineffective. The ligand L was characterized by H-1 NMR, FTIR and HRMS spectral techniques. UV-Visible spectroscopic technique was used to study the sensing ability of probe L for copper ions above other metal ions. The Job’s plot obtained from absorption studies and HRMS data confirmed that the Cu2+ ions bind with ligand L in 1:1 stoichiometric ratio. DFT computations were also supported the binding framework between L and Cu (II) ions. The LOD value and the association constant were obtained 3.9 x 10(-7) M and 2.3 x 10(5) M-1 respectively, via Benesi-Hildebrand equation. Selectivity of L towards Cu2+ ions was also studied and it was found that the probe L worked specifically for copper ions without any considerable influence of other intruding metal ions. In addition, in real water samples, the ligand L was fully implemented for identification and quantification of Cu2+ ions. (C) 2020 Elsevier B.V. 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.. Computed Properties of C5H4N2O2

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

Formula: C5H4N2O2. In 2020 J ORGANOMET CHEM published article about TRANSFER HYDROGENATION; ALPHA-ALKYLATION; RUTHENIUM(II) COMPLEXES; PRIMARY ALCOHOLS; KETONES; IRIDIUM; DEHYDROGENATION; REACTIVITY; SECONDARY; BEARING in [Pakyapan, Bilge; Kavukcu, Serdar Batikan; Turkmen, Hayati] Univ Ege, Fac Sci, Dept Chem, TR-35100 Izmir, Turkey; [Sahin, Zarife Sibel] Univ Sinop, Sci & Technol Res Applicat & Res Ctr, Sinop, Turkey in 2020, Cited 44. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A series of monometallic complexes (Ru1-3, Ir-1(-3)) which have N,O-chelating ligand (pyrazine-2carboxylate (1), pyridine-2-carboxylate (2), quinoline carboxylate(3) and bimetallic complexes (Ru-4,Ru-5, Ir-4(,5)) bridged by pyrazine-2,3- dicarboxylate (4) and imidazole-4,5-dicarboxylate(5) were synthesized and characterized by H-1-, C-13 NMR, FT-IR, and elemental analysis. The crystal structure of Ir-2 was determined by X-ray crystallography. The complexes (Ru1-5, Ir1-5) were applied to investigate the electronic and steric effect of ligand in their catalytic activities in transfer hydrogenation and alpha(alpha)-alkylation reaction of ketones with alcohols. The activities of iridium complexes (Ir1-5) were much more efficient than ruthenium complexes (Ru1-5). The highest activity for both reactions was observed for the complex (Ir2 ) with pyridine-2-carboxylate. The Ir hydride species was monitored for both reactions. (C) 2020 Elsevier B.V. All rights reserved.

Welcome to talk about 98-97-5, If you have any questions, you can contact Pakyapan, B; Kavukcu, SB; Sahin, ZS; Turkmen, H or send Email.. Formula: C5H4N2O2

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

Recommanded Product: Pyrazine-2-carboxylic acid. In 2019 CHEM-EUR J published article about CARBOXYLIC-ACIDS; DIRECT AMIDATION; AMIDE SYNTHESIS; ESTERS; ALPHA; INHIBITORS; CHEMISTRY in [Opie, Christopher R.; Noda, Hidetoshi; Shibasaki, Masakatsu; Kumagai, Naoya] Inst Microbial Chem BIKAKEN, Shinagawa Ku, 3-14-23 Kamiosaki, Tokyo 1410021, Japan in 2019, Cited 63. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

The B3NO2 six-membered heterocycle (1,3-dioxa-5-aza-2,4,6-triborinane = DATB), comprising three different non-carbon period 2 elements, has been recently demonstrated to be a powerful catalyst for dehydrative condensation of carboxylic acids and amines. The tedious synthesis of DATB, however, has significantly diminished its utility as a catalyst, and thus the inherent chemical properties of the ring system have remained virtually unexplored. Here, a general and facile synthetic strategy that harnesses a pyrimidine-containing scaffold for the reliable installation of boron atoms is disclosed, giving rise to a series of Pym-DATBs from inexpensive materials in a modular fashion. The identification of a soluble Pym-DATB derivative allowed for the investigation of the dynamic nature of the B3NO2 ring system, revealing differential ring-closing and -opening behaviors depending on the medium. Readily accessible Pym-DATBs proved their utility as efficient catalysts for dehydrative amidation with broad substrate scope and functional-group tolerance, offering a general and practical catalytic alternative to reagent-driven amidation.

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: Pyrazine-2-carboxylic acid

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

An article Mycobacterium tuberculosis PanD Structure-Function Analysis and Identification of a Potent Pyrazinoic Acid-Derived Enzyme Inhibitor WOS:000664331200009 published article about ASPARTATE-ALPHA-DECARBOXYLASE; PYRAZINAMIDE RESISTANCE; CRYSTAL-STRUCTURE; ATP SYNTHESIS; MUTATIONS; EXPRESSION; SYNTHASE in [Ragunathan, Priya; Latka, Chitra; Shin, Joon; Manimekalai, Malathy Sony Subramanian; Rishikesan, Sankaranarayanan; Gruber, Gerhard] Nanyang Technol Univ, Sch Biol Sci, Singapore 637551, Singapore; [Cole, Malcolm; Hegde, Pooja; Aldrich, Courtney C.] Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA; [Aragaw, Wassihun Wedajo; Dick, Thomas] Hackensack Meridian Hlth, Ctr Discovery & Innovat, Nutley, NJ 07110 USA; [Dick, Thomas] Hackensack Meridian Sch Med, Dept Med Sci, Nutley, NJ 07110 USA; [Dick, Thomas] Georgetown Univ, Dept Microbiol & Immunol, Washington, DC 20007 USA in 2021, Cited 28. 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 common strategy employed in antibacterial drug discovery is the targeting of biosynthetic processes that are essential and specific for the pathogen. Specificity in particular avoids undesirable interactions with potential enzymatic counterparts in the human host, and it ensures ontarget toxicity. Synthesis of pantothenate (Vitamine B5), which is a precursor of the acyl carrier coenzyme A, is an example of such a pathway. In Mycobacterium tuberculosis (Mtb), which is the causative agent of tuberculosis (TB), pantothenate is formed by pantothenate synthase, utilizing D-pantoate and beta-Ala as substrates. beta-Ala is mainly formed by the decarboxylation of L-aspartate, generated by the decarboxylase PanD, which is a homo-oliogomer in solution. Pyrazinoic acid (POA), which is the bioactive form of the TB prodrug pyrazinamide, binds and inhibits PanD activity weakly. Here, we generated a library of recombinant Mtb PanD mutants based on structural information and PZA/POA resistance mutants. Alterations in oligomer formation, enzyme activity, and/or POA binding were observed in respective mutants, providing insights into essential amino acids for Mtb PanD’s proper structural assembly, decarboxylation activity and drug interaction. This information provided the platform for the design of novel POA analogues with modifications at position 3 of the pyrazine ring. Analogue 2, which incorporates a bulky naphthamido group at this position, displayed a 1000-fold increase in enzyme inhibition, compared to POA, along with moderately improved antimycobacterial activity. The data demonstrate that an improved understanding of mechanistic and enzymatic features of key metabolic enzymes can stimulate design of more-potent PanD inhibitors.

Welcome to talk about 98-97-5, If you have any questions, you can contact Ragunathan, P; Cole, M; Latka, C; Aragaw, WW; Hegde, P; Shin, J; Manimekalai, MSS; Rishikesan, S; Aldrich, CC; Dick, T; Gruber, G or send Email.. Recommanded Product: 98-97-5

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

Authors Han, JF; Wang, K; You, GR; Wang, GD; Sun, J; Duan, GY; Xia, CC in ELSEVIER published article about ONE-POT SYNTHESIS; H FUNCTIONALIZATION; ACTIVATION; SULFONYLATION; C(SP(2))-H; SODIUM in [Han, Junfen; Wang, Kai; You, Guirong; Wang, Guodong; Sun, Jian; Duan, Guiyun; Xia, Chengcai] Shandong First Med Univ & Shandong Acad Med Sci, Coll Pharm, Tai An 271000, Shandong, Peoples R China in 2019, Cited 35. Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

A novel and regioselective protocol for C-S coupling of naphthylamines via the insertion of sulfur dioxide was developed by employing a heterogeneous copper catalyst, providing desired products in moderate to good yields. This strategy gives a powerful tool for the efficient preparation of sulfur-containing compounds. Control experiments declared that a single-electron transfer mechanism (SET) is responsible for this C-S cross coupling reaction.

Formula: C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Han, JF; Wang, K; You, GR; Wang, GD; Sun, J; Duan, GY; Xia, CC or send Email.

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

Name: Pyrazine-2-carboxylic acid. Ju, Y; He, LH; Zhou, YZ; Yang, T; Sun, K; Song, R; Yang, Y; Li, CW; Sang, ZT; Bao, R; Luo, YF in [Ju, Yuan; He, Lihui; Zhou, Yuanzheng; Yang, Tao; Sun, Ke; Song, Rao; Yang, Yang; Li, Chengwei; Bao, Rui; Luo, Youfu] Sichuan Univ, State Key Lab Biotherapy, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China; [Ju, Yuan; He, Lihui; Zhou, Yuanzheng; Yang, Tao; Sun, Ke; Song, Rao; Yang, Yang; Li, Chengwei; Bao, Rui; Luo, Youfu] Sichuan Univ, Canc Ctr, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China; [Sang, Zitai] Luoyang Normal Univ, Inst Life Sci, Luoyang 471934, Henan, Peoples R China published Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers in Vitro and in Vivo in 2020, Cited 53. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

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.

Name: Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, 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 send Email.

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