Category: 98-97-5

Name: Pyrazine-2-carboxylic acid. Recently I am researching about MECHANISMS; IDENTIFICATION; INFLAMMASOME; CHEMOTAXIS, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81573278, 81773745]; Excellent Science and Technology Innovation Team Projects of Jiangsu Province Universities in 2018; Double First-Class University project [CPU2018GF02]. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Zhang, ZG; Hao, K; Li, HW; Lu, R; Liu, CX; Zhou, MZ; Li, BY; Meng, ZB; Hu, QH; Jiang, C. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

The P2Y(14) receptor (P2Y(14)R) plays a key role in the modulation of inflammatory process, but very few classes of antagonists have been reported. A series of 3-amide benzoic acid derivatives were identified as novel and potent P2Y(14)R antagonists. The most potent antagonist, 16c, showed comparable activity (IC50 = 1.77 nM) to PPTN, the most potent P2Y(14)R antagonist reported. Compound 16c demonstrated dramatically improved aqueous solubility and excellent metabolic stability in rat and human microsomes. Investigation of the anti-inflammatory effect of 16c was performed in MSU treated THP-1 cells by flow cytometry, Western Blot and immunofluorescence labeling technology, which exhibited that 16c might be a promising candidate for further research. (C) 2019 Elsevier Masson SAS. All rights reserved.

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

In 2021 ACS CHEM BIOL 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. Name: Pyrazine-2-carboxylic acid

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.. Name: Pyrazine-2-carboxylic acid

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

Authors Wang, ZG; Yan, XJ; Liu, HB; Zhang, DL; Liu, W; Xie, CZ; Li, QZ; Xu, JY in ROYAL SOC CHEMISTRY 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.

Recommanded Product: 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

Authors Pandolfi, F; D’Acierno, F; Bortolami, M; De Vita, D; Gallo, F; De Meo, A; Di Santo, R; Costi, R; Simonetti, G; Scipione, L in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about ACID-DERIVATIVES; IN-VIVO in [Pandolfi, Fabiana; Bortolami, Martina; De Vita, Daniela; Gallo, Fabio; De Meo, Alessandra; Scipione, Luigi] Sapienza Univ Rome, Dept Chim & Tecnol Farmaco, Piazzale Aldo Moro 5, I-00185 Rome, Italy; [D’Acierno, Federica; Simonetti, Giovanna] Sapienza Univ Rome, Dept Sanita Pubbl & Malattie Infett, Piazzale Aldo Moro 5, I-00185 Rome, Italy; [Di Santo, Roberto; Costi, Roberta] Sapienza Univ Rome, Ist Pasteur Fdn Cenci Bolognetti, Dept Chim & Tecnol Farmaco, Piazzale Aldo Moro 5, I-00185 Rome, Italy in 2019, Cited 29. COA of Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Candida albicans biofilm represents a major clinical problem due to its intrinsic tolerance to anti-fungal compounds and it has been highly related to infections in catheterized patients. Few compounds are described as able to inhibit biofilm formation or to interfere with preformed biofilm of C. albicans. Here we report the in vitro evaluation of anti-biofilm activity on C albicans ATCC 10231 of a series of new and already known amine and amide indole derivatives. Among the studied compounds, fifteen resulted active on C albicans ATCC 10231 biofilm, with BMIC50 <= 16 mu g/mL. Three of them (7, 23 and 33) showed a selectivity towards mature biofilm and the most active of them was the compound 23 (BMIC50 = 4 mu g/mL). On the other hands, two different compounds (21 and 22) were selective towards biofilm formation with BMIC50 values of 8 mu g/mL Otherwise, compounds 16 and 17 resulted active on biofilm formation, with BMIC50 of 8 mu g/mL and 2 mu g/mL respectively, and on mature biofilm with BMIC50 of 2 mu g/mL. These two last compounds also showed an interesting activity towards the planktonic cells of C albicans. A selection of the more active compounds was also evaluated on different C albicans strains (PMC1042, PMC1083 and ATCC 10261), showing a comparable or higher anti-biofilm activity, especially on mature biofilm. In vivo toxicity studies using the Galleria mellonella larvae, were finally carried out on more active indole derivatives, showing that they are poorly toxic even at the highest concentrations tested (500-1000 mu g/mL). (C) 2019 Elsevier Masson SAS. All rights reserved. COA of Formula: C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Pandolfi, F; D’Acierno, F; Bortolami, M; De Vita, D; Gallo, F; De Meo, A; Di Santo, R; Costi, R; Simonetti, G; Scipione, L or send Email.

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

COA of Formula: C5H4N2O2. In 2019 EUR J MED CHEM published article about BIOLOGICAL EVALUATION; MOLECULAR DOCKING; 20S PROTEASOME; DESIGN; DERIVATIVES; IDENTIFICATION; DEGRADATION; GENERATION; APOPTOSIS; MYELOMA in [Dong, Xiao-Wu; Zhang, Jian-Kang; Che, Jin-Xin; Liu, Tao; Hu, Yong-Zhou] Zhejiang Univ, ZJU ENS Joint Lab Med Chem, Zhejiang Prov Key Lab Anticanc Drug Res, Hangzhou Inst Innovat Med,Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China; [Xu, Lei; Hu, Xiao-Bei; Sheng, Li; Gao, An-Hui; Li, Jia; Liu, Tao; Zhou, Yu-Bo] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; [Xu, Lei; Hu, Xiao-Bei; Sheng, Li; Gao, An-Hui; Li, Jia; Zhou, Yu-Bo] Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China; [Zhang, Jian-Kang] Zhejiang Univ City Coll, Sch Med, Hangzhou 310015, Zhejiang, Peoples R China; [Cheng, Gang] Zhejiang Chinese Med Univ, Coll Pharmaceut Sci, Hangzhou 311402, Zhejiang, Peoples R China in 2019, Cited 33. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

The potential of specific proteasome inhibitors to act as anti-cancer agents has attracted intensive investigations. The proteasome can be covalently inhibited by epoxyketone derivatives via a two-step reaction. Several computational approaches have been developed to mimic the covalent binding event. Compound 1 composed of a six-membered heterocyclic ring was designed by using covalent docking. With a possible different binding mode from the clinical compound Carfilzomib, it occupied the 55 pocket of 20S proteasome and showed favorable inhibitory activity. Subsequently optimization and evaluation were taken place. Among these compounds, 11h demonstrated extraordinary in vitro inhibitory activity and selectivity, and good in vivo proteasome inhibitory activity, a favorable pharmacokinetic profile and xenograft tumor inhibition. The possible binding pattern of compound 11h against proteasome was further fully explored via calculations, providing a theoretical basis for finding potent proteasome inhibitors. (C) 2018 Elsevier Masson SAS. All rights reserved.

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

In 2021 BIOORG CHEM published article about RESISTANCE; ANTIBIOTICS; ANIMALS 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 in 2021, Cited 29. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Formula: C5H4N2O2

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.

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

Recently I am researching about MYCOBACTERIUM; DRUG; RESISTANCE; DELAMANID; DISCOVERY; MECHANISMS; INHIBITORS; ASSAY; Q203; BCG, Saw an article supported by the Durham University; Newcastle University. Recommanded Product: 98-97-5. Published in MDPI in BASEL ,Authors: Brown, AK; Aljohani, AKB; Alsalem, FMA; Broadhead, JL; Gill, JH; Lu, YC; Sellars, JD. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Discovery and development of new therapeutic options for the treatment of Mycobacterium tuberculosis (Mtb) infection, particularly drug-resistant strains, are urgently required to tackle the global burden of this disease. Herein, we reported the synthesis of a novel series of N-substituted amino acid hydrazides, utilising a scaffold hopping approach within a library of anti-tubercular agents. Efficacy and selectivity were evaluated against three strains of Mtb (wild-type, isoniazid-resistant and rifampicin-resistant), and cytotoxicity against macrophages in vitro. The antibacterial activity and therapeutic index of these molecules were significantly affected by modifications with the N-substituents. Introduction of a 3,5-dinitroaryl moiety demonstrated enhanced antibacterial activity against all three strains of Mtb. In contrast, the inclusion of an imidazo [1,2-a]pyridine-3-carboxy moiety resulted in enhanced activity towards isoniazid mono-resistant Mtb relative to wild-type Mtb. Consequently, this scaffold hopping approach showed significant promise for exemplification of novel molecules with specific activity profiles against drug-resistant tuberculosis.

Welcome to talk about 98-97-5, If you have any questions, you can contact Brown, AK; Aljohani, AKB; Alsalem, FMA; Broadhead, JL; Gill, JH; Lu, YC; Sellars, JD or send Email.. Recommanded Product: 98-97-5

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

Recently I am researching about CRYSTAL-STRUCTURE; 20S PROTEASOME; ALPHA; EXPRESSION; BORTEZOMIB; SUBSTRATE; DOCKING, Saw an article supported by the DFGGerman Research Foundation (DFG)European Commission [GRK1657]. Formula: C5H4N2O2. Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Stubba, D; Bensinger, D; Steinbacher, J; Proskurjakov, L; Gomez, AS; Schmidt, U; Roth, S; Schmitz, K; Schmidt, B. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

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.

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

Safety of Pyrazine-2-carboxylic acid. In 2019 J AM CHEM SOC published article about DIRECTING GROUPS; MOLECULAR I-2; BONDS; FUNCTIONALIZATION; HALOGENATION; ALKYLATION; C(SP(3))-H; ARYLATION; MILD; ALLYLAMINES in [Schreib, Benedikt S.; Carreira, Erick M.] Swiss Fed Inst Technol, HCI, Vladimir Prelog Weg 3, CH-8093 Zurich, Switzerland in 2019, Cited 63. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A palladium-catalyzed C-H iodination of unactivated alkenes is reported. A picolinamide directing group enables the regioselective functionalization of a wide array of olefins to furnish iodination products as single stereoisomers. Mechanistic investigations suggest the reversible formation of a six-membered alkenyl palladacycle intermediate through a turnover-limiting C-H activation.

Safety of 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 Seeking potent anti-tubercular agents: design and synthesis of substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives as anti-tubercular agents WOS:000526839700017 published article about MYCOBACTERIUM-TUBERCULOSIS; ANTIMYCOBACTERIAL EVALUATION; IN-VITRO; DOCKING; ANALOGS in [Srinivasarao, Singireddi; Nandikolla, Adinarayana; Suresh, Amaroju; Aggarwal, Himanshu; Sekhar, Kondapalli Venkata Gowri Chandra] Birla Inst Technol & Sci, Dept Chem, Hyderabad Campus, Hyderabad 500078, Telangana, India; [Calster, Kevin Van; De Voogt, Linda; Cappoen, Davie] Univ Ghent, Fac Biosci Engn, Dept Green Chem & Technol, Coupure Links 653, B-9000 Ghent, Belgium; [Ghosh, Balaram] Birla Inst Technol & Sci, Dept Pharm, Hyderabad Campus, Hyderabad 500078, Telangana, India; [Murugesan, Sankaranarayanan] Birla Inst Technol & Sci, Dept Pharm, Med Chem Res Lab, Pilani 333031, Rajasthan, India in 2020, Cited 34. 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

Pyrazinamide is an important first-line drug used in shortening TB therapy. In our current work, a series of novel substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives were designed, synthesized, and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Ra. Among the tested compounds, five compounds (6a, 6e, 6h, 6j and 6k) from Series-I and one compound (7e) from Series-II exhibited significant activity against Mycobacterium tuberculosis H37Ra with 50% inhibitory concentrations (IC50) ranging from 1.35 to 2.18 mu M. To evaluate the efficacy of these compounds, we examined their IC90 values. Five of the most active compounds were found to be more active with IC(90)s ranging from 3.73 to 4.00 mu M and one compound (6e) showed an IC90 of 40.32 mu M. Moreover, single crystals were developed for 6d, 6f and 6n. In addition, most active compounds were evaluated for their cytotoxicity on HEK-293 (human embryonic kidney) cells. Our results indicate that the compounds are nontoxic to human cells. The molecular interactions of the derivatised conjugates in docking studies reveal their suitability for further development.

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