Month: December 2021

SDS of cas: 98-97-5. Recently I am researching about OXIDIZED PROTEIN HYDROLASE; SERINE PROTEASES; IRREVERSIBLE INHIBITION; DERIVATIVES; ACID; IDENTIFICATION; ACETYLATION; DESIGN; GROWTH; ESTERS, Saw an article supported by the National Science Center NCN – Preludium [5 DEC-2013/09/N/ST5/02472]; Wrocaw University of Science and Technology. Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Walczak, M; Chryplewicz, A; Olewinska, S; Psurski, M; Winiarski, L; Torzyk, K; Oleksyszyn, J; Sienczyk, M. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Acylpeptide hydrolase is a serine protease, which, together with prolyl oligopeptidase, dipeptidyl peptidase IV and oligopeptidase B, belongs to the prolyl oligopeptidase family. Its primary function is associated with the removal of N-acetylated amino acid residues from proteins and peptides. Although the N-acylation occurs in 50-90 % of eukaryotic proteins, the precise functions of this modification remains unclear. Recent findings have indicated that acylpeptide hydrolase participates in various events including oxidized proteins degradation, amyloid beta-peptide cleavage, and response to DNA damage. Considering the protein degradation cycle cross-talk between acylpeptide hydrolase and proteasome, inhibition of the first enzyme resulted in down-regulation of the ubiquitin-proteasome system and induction of cancer cell apoptosis. Acylpeptide hydrolase has been proposed as an interesting target for the development of new potential anticancer agents. Here, we present the synthesis of simple derivatives of (1-aminoethyl)phosphonic acid diaryl esters, phosphonic analogs of alanine diversified at the N-terminus and ester rings, as inhibitors of acylpeptide hydrolase and discuss the ability of the title compounds to induce apoptosis of U937 and MV-4-11 tumor cell lines.

SDS of cas: 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Walczak, M; Chryplewicz, A; Olewinska, S; Psurski, M; Winiarski, L; Torzyk, K; Oleksyszyn, J; Sienczyk, M or send Email.

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

Quality Control of Pyrazine-2-carboxylic acid. In 2019 MOL NUTR FOOD RES published article about 5-HYDROXYPYRAZINOIC ACID; NICOTINIC-ACID; RAT; CONSUMPTION; MECHANISM; PLASMA; URINE in [Kremer, Jonathan I.; Pickard, Stephanie; Stadlmair, Lara F.; Glass-Theis, Anika; Buckel, Leon; Bakuradze, Tamara; Eisenbrand, Gerhard; Richling, Elke] Tech Univ Kaiserslautern, Dept Chem, Div Food Chem & Toxicol, Erwin Schrodinger Str 52, D-67663 Kaiserslautern, Germany in 2019, Cited 33. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

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.

Welcome to talk about 98-97-5, 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 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. I found the field of Environmental Sciences & Ecology very interesting. Saw the article Experimental and theoretical approach to probe the aquatic speciation of transuranic (neptunyl) ion in presence of two omnipresent organic moieties published in 2021, Reprint Addresses Dumpala, RMR (corresponding author), Bhabha Atom Res Ctr, Radio Chem Div, Mumbai 400094, Maharashtra, India.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid.

Pyrazines are omnipresent in nature and have their occurrence in plants, microbes, food supplies, marine arenas. The present studies aimed at aquatic speciation of the neptunyl ion (NpO2+) with two pyrazine compounds namely pyrazine monocarboxylic acid (PMC) and pyrazine dicarboxylic acid (PDC). Absorption spectrophotometry was used to probe the stability, speciation and spectral properties for the complexation process. NpOO2+ forms a more stable complex with PMC than PDC for 1:1 (ML), while for 1:2 (ML2) the opposite trend is observed. The extent of shift in lambda(max), which is also an indicator for the strength of complexation, reflected similar trends for the complexation process. Isothermal titration calorimetry was employed to determine the enthalpies of complex formation, which is found to be endothermic. The complexation process is entropy driven. Linear free energy correlations were established to retrieve the coordination modes of the complexes. The variation in peak potentials (the cyclic voltammograms) with change in pH and metal to ligand ratio were explored to understand redox speciation, electron transfer kinetics and Eh-pH characteristics for the interaction of NpOO2+ with pyrazine carboxylate ligands. Density functional theory calculations were employed to optimize the geometries and to calculate the bond distances and partial charges on key atoms of the optimized geometries. The theoretical calculations helped to reveal the contributions from two different configurations of the same geometry towards the optical absorption. The bond distances and partial charges estimated theoretically helped to understand the aqueous interactions at the molecular level. (C) 2021 Elsevier Ltd. All rights reserved.

Welcome to talk about 98-97-5, If you have any questions, you can contact Dumpala, RMR; Srivastava, A; Rawat, N or send Email.. Product Details of 98-97-5

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. 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 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.

Recommanded Product: 98-97-5. 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.

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

Category: Pyrazines. Recently I am researching about HIGHLY EFFICIENT; METAL-COMPLEXES; QUINOXALINE LIGANDS; 1ST EXAMPLES; PHOSPHORESCENT; EMISSION; BEARING; PHOTOPHYSICS; CONVERSION; DEVICES, Saw an article supported by the Cardiff University (Knowledge Economy Skills Scholarship); STG Aerospace; Engineering and Physical Sciences Research Council (EPSRC)UK Research & Innovation (UKRI)Engineering & Physical Sciences Research Council (EPSRC) [EP/L504749/1]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Stonelake, TM; Phillips, KA; Otaif, HY; Edwardson, ZC; Horton, PN; Coles, SJ; Beames, JM; Pope, SJA. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

A series of heteroleptic, neutral iridium(III) complexes of the form [Ir(L)(2)(N boolean AND O)] (where L = cyclometalated 2,3-disubstituted quinoxaline and N boolean AND O = ancillary picolinate or pyrazinoate) are described in terms of their synthesis and spectroscopic properties, with supporting computational analyses providing additional insight into the electronic. properties. The 10 [Ir(L)(2)(N boolean AND O)] complexes were characterized using a range of analytical techniques (including H-1, C-13, and F-19 NMR and IR spectroscopies and mass spectrometry). One of the examples was structurally characterized using X-ray diffraction. The redox properties were determined using cyclic voltammetry, and the electronic properties were investigated using UV-vis, time-resolved luminescence, and transient absorption spectroscopies. The complexes are phosphorescent in the red region of the visible spectrum (lambda(em) = 633-680 nm), with lifetimes typically of hundreds of nanoseconds and quantum yields ca. 5% in aerated chloroform. A combination of spectroscopic and computational analyses suggests that the long-wavelength absorption and emission properties of these complexes are strongly characterized by a combination of spin-forbidden metal-to-ligand charge-transfer and quinoxaline-centered transitions. The emission wavelength in these complexes can thus be controlled in two ways: first, substitution of the cyclometalating quinoxaline ligand can perturb both the highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital levels (LUMO, Cl atoms on the ligand induce the largest bathochromic shift), and second, the choice of the ancillary ligand can influence the HOMO energy (pyrazinoate stabilizes the HOMO, inducing hypsochromic shifts).

Category: Pyrazines. 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 Wang, JW; Hong, G; Li, GL; Wang, WZ; Liu, TJ in MDPI 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. 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

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.

Name: Pyrazine-2-carboxylic acid. 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.

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

Recommanded Product: 98-97-5. Authors Ma, JJ; Chen, SM; Bellotti, P; Guo, RY; Schafer, F; Heusler, A; Zhang, XL; Daniliuc, C; Brown, MK; Houk, KN; Glorius, F in AMER ASSOC ADVANCEMENT SCIENCE published article about in [Ma, Jiajia; Bellotti, Peter; Schafer, Felix; Heusler, Arne; Zhang, Xiaolong; Daniliuc, Constantin; Glorius, Frank] Westfalische Wilhelms Univ Munster, Organ Chem Inst, Corrensstr 40, D-48149 Munster, Germany; [Chen, Shuming; Houk, Kendall N.] Univ Calif Los Angeles, Dept Chem & Biochem, Los Angeles, CA 90095 USA; [Guo, Renyu; Brown, M. Kevin] Indiana Univ, Dept Chem, Bloomington, IN 47405 USA in 2021, Cited 74. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Dearomative cycloaddition reactions represent an ideal means of converting flat arenes into three-dimensional architectures of increasing interest in medicinal chemistry. Quinolines, isoquinolines, and quinazolines, despite containing latent diene and alkene subunits, are scarcely applied in cycloaddition reactions because of the inherent low reactivity of aromatic systems and selectivity challenges. Here, we disclose an energy transfer-mediated, highly regio- and diastereoselective intermolecular [4 + 2] dearomative cycloaddition reaction of these bicyclic azaarenes with a plethora of electronically diverse alkenes. This approach bypasses the general reactivity and selectivity issues, thereby providing various bridged polycycles that previously have been inaccessible or required elaborate synthetic efforts. Computational studies with density functional theory elucidate the mechanism and origins of the observed regio- and diastereoselectivities.

Recommanded Product: 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Ma, JJ; Chen, SM; Bellotti, P; Guo, RY; Schafer, F; Heusler, A; Zhang, XL; Daniliuc, C; Brown, MK; Houk, KN; Glorius, F or send Email.

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

Authors Stubba, D; Bensinger, D; Steinbacher, J; Proskurjakov, L; Gomez, AS; Schmidt, U; Roth, S; Schmitz, K; Schmidt, B in WILEY-V C H VERLAG GMBH published article about CRYSTAL-STRUCTURE; 20S PROTEASOME; ALPHA; EXPRESSION; BORTEZOMIB; SUBSTRATE; DOCKING in [Stubba, Daniel; Bensinger, Dennis; Steinbacher, Janika; Proskurjakov, Lilia; Gomez, Alvaro Salcedo; Schmitz, Katja; Schmidt, Boris] Tech Univ Darmstadt, Clemens Schoepf Inst Organ Chem & Biochem, Alarich Weiss Str 4, D-64287 Darmstadt, Germany; [Schmidt, Uwe; Roth, Stefan] Tech Univ Darmstadt, Dept Comp Sci, Visual Inference Lab, Huchschulstr 10, D-64289 Darmstadt, Germany in 2019, Cited 42. 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 ubiquitin-proteasome system (UPS) is an established therapeutic target for approved drugs to treat selected hematologic malignancies. While drug discovery targeting the UPS focuses on irreversibly binding epoxyketones and slowly-reversibly binding boronates, optimization of novel covalent-reversibly binding warheads remains largely unattended. We previously reported alpha-ketoamides to be a promising reversible lead motif, yet the cytotoxic activity required further optimization. This work focuses on the lead optimization of phenoxy-substituted alpha-ketoamides combining the structure-activity relationships from the primed and the non-primed site of the proteasome beta 5 subunit. Our optimization strategy is accompanied by molecular modeling, suggesting occupation of P1 ‘ by a 3-phenoxy group to increase beta 5 inhibition and cytotoxic activity in leukemia cell lines. Key compounds were further profiled for time-dependent inhibition of cellular substrate conversion. Furthermore, the alpha-ketoamide lead structure 27 does not affect escape response behavior in Danio rerio embryos, in contrast to bortezomib, which suggests increased target specificity.

Product Details of 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Stubba, D; Bensinger, D; Steinbacher, J; Proskurjakov, L; Gomez, AS; Schmidt, U; Roth, S; Schmitz, K; Schmidt, B or send Email.

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

In 2020 BIOORG CHEM published article about MYCOBACTERIUM-TUBERCULOSIS; ANTIMYCOBACTERIAL ACTIVITY; ACID HYDRAZONES; DERIVATIVES; RESISTANCE; DOCKING; DRUGS; GRANULOCYTES; INHIBITORS; PREDICTION in [Hassan, Nayera W.; Saudi, Manal N.; Abdel-Ghany, Yasser S.; Ismail, Azza; Elzahhar, Perihan A.; El-Hawash, Soad A.] Alexandria Univ, Fac Pharm, Dept Pharmaceut Chem, Alexandria 21521, Egypt; [Sriram, Dharmarajan] Birla Inst Technol & Sci Pilani, Med Chem & Drug Discovery Res Lab, Pharm Grp, Hyderabad Campus, Jawahar Nagar 500078, Telangana, India; [Nassra, Rasha] Alexandria Univ, Fac Med, Dept Med Biochem, Alexandria, Egypt; [Abdel-Aziz, Marwa M.] Al Azhar Univ, Reg Ctr Mycol & Biotechnol, Cairo 11759, Egypt in 2020, Cited 84. 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

TB continues to be a leading health threat despite the availability of powerful anti-TB drugs. We report herein the design and synthesis of various hybrid molecules comprising pyrazine scaffold and various formerly identified anti-mycobacterial moieties. Thirty-one compounds were screened in vitro for their activity against Mycobacterium tuberculosis H37Rv strain using MABA assay. The results revealed that six compounds (8a, 8b, 8c, 8d, 14b and 18) displayed significant activity against Mtb with MIC values <= 6.25 mu g/ml versus 6.25 mu g/ml for pyrazinamide. The most active compounds were then assessed for their in vitro cytotoxicity against PBMC normal cell line using MTT assay and showed SI > 200. Several in silico studies have been carried out for target fishing of the novel compounds such as shape-based similarity, pharmacophore mapping and inverse docking. Based on this multi-step target fishing study, we suggest that pantothenate synthetase could be the possible target responsible for the action of these compounds. The most active compounds were then successfully docked into the active site of pantothenate synthetase enzyme with favorable binding interactions. In addition, in silico prediction of physicochemical, ADMET and drug-like properties were also determined indicating that compounds 8b, 8c and 8d are promising candidates for the development of new anti-TB agents with enhanced activity and better safety profile.

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

Recommanded Product: 98-97-5. Recently I am researching about MYCOBACTERIUM-TUBERCULOSIS; ANTIBACTERIAL ACTIVITY; RAMAN-SPECTROSCOPY; CONTROLLED-RELEASE; HYBRID MATERIALS; GRAPHITE; DELIVERY; NANOMATERIALS; CYTOTOXICITY; DOXORUBICIN, Saw an article supported by the EU (ERDF)European Commission [INFRANANOCHEM19/01.03.2009]; Romanian Government [INFRANANOCHEM19/01.03.2009]. Published in ELSEVIER SCIENCE BV in AMSTERDAM ,Authors: Tudos, M; Anghel, EM; Culita, DC; Somacescu, S; Calderon-Moreno, J; Tecuceanu, V; Dumitrascu, FD; Dracea, O; Popa, M; Marutescu, L; Bleotu, C; Curutiu, C; Chifiriuc, MC. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

In this work, we present a simple, two-stage method for the preparation of new and efficient antimicrobial hybrid systems, based on isoniazid and pyrazine-2-carbohydrazide tuberculostatic agents covalently linked to graphene oxide. In the first step, the carboxyl groups of graphene oxide are activated by transforming them into the corresponding acid chloride groups, which, in the second step, will react with the amino groups of the two drugs. Pyrazine-2-carbohydrazide was obtained from pyrazinoic acid and hydrazine hydrate and was confirmed by nuclear magnetic resonance spectroscopy. The materials have been characterized by elemental analysis, infrared spectroscopy, Raman spectroscopy, scanning electron microscopy, and X-ray photoelectron spectroscopy. Their antimicrobial activity was tested on mycobacterial (Mycobacterium terrae), as well as on Gram-negative bacteria (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853), Gram-positive bacteria (Staphylococcus aureus ATCC 6538, Staphylococcus aureus ATCC 25923) and fungal (Candida albicans ATCC 10231), in planktonic and biofilm growth state. The biocompatibility of the tested compounds was assessed in vitro by live-dead fluorescence staining and flow cytometry. The results of this study have shown that the functionalization of graphene oxide with isoniazid and pyrazine-2-carbohydrazide both enhanced the anti-mycobacterial activity of the respective drugs and extended their antimicrobial spectrum towards other microbial strains, in planktonic and biofilm growth state, showing a promising potential for mitigating the impact of antimicrobial resistance and the deleterious effects of microbial biofilms. At the active tuberculostatic concentrations, the tested compounds exhibit very low cytotoxicity and do not interfere with the cellular cycle of Hep-2 cells. The flow cytometry and live/dead fluorescence staining proved that the tested compounds exhibit a microbicidal effect through induction of cellular lesions, consecutive to membrane depolarization.

Welcome to talk about 98-97-5, If you have any questions, you can contact Tudos, M; Anghel, EM; Culita, DC; Somacescu, S; Calderon-Moreno, J; Tecuceanu, V; Dumitrascu, FD; Dracea, O; Popa, M; Marutescu, L; Bleotu, C; Curutiu, C; Chifiriuc, MC or send Email.. Recommanded Product: 98-97-5

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