Month: November 2021

Lei, JC; Ruan, YX; Luo, S; Yang, JS in [Lei, Jin-Cai; Ruan, Yu-Xiong; Luo, Sheng; Yang, Jin-Song] Sichuan Univ, West China Hosp, Key Lab Drug Targeting & Drug Delivery Syst, Sichuan Engn Lab Plant Sourced Drug,Educ Minist, Chengdu 610041, Sichuan, Peoples R China; [Lei, Jin-Cai; Ruan, Yu-Xiong; Luo, Sheng; Yang, Jin-Song] Sichuan Univ, West China Hosp, West China Sch Pharm, Sichuan Res Ctr Drug Precis Ind Technol, Chengdu 610041, Sichuan, Peoples R China; [Lei, Jin-Cai; Ruan, Yu-Xiong; Luo, Sheng; Yang, Jin-Song] Sichuan Univ, West China Hosp, State Key Lab Biotherapy, Chengdu 610041, Sichuan, Peoples R China published Stereodirecting Effect of C3-Ester Groups on the Glycosylation Stereochemistry of L-Rhamnopyranose Thioglycoside Donors: Stereoselective Synthesis of alpha- and beta-L-Rhamnopyranosides in 2019, Cited 47. 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.

The tuning effect of C3-ester groups on the glycosylation stereochemistry of L-rhamnopyranose (L-Rha) ethyl thioglycoside donors is described. On one hand, the L-Rha thioglycoside donors carrying 3-O-arylcarbonyl or levulinoyl group undergo highly alpha-selective glycosylation to afford a wide variety of alpha-L-rhamnoside products in high chemical yields. On the other hand, the glycosylation of the 3-O-4-nitropicoloyl and 2-pyrazinecarbonyl group substituted L-Rha thioglycosides displays beta-stereoselectivity. Only or predominant beta anomeric products are obtained when these L-Rha donors couple with the primary or reactive secondary acceptors, while the beta-selectivity may decrease significantly when these donors react with less reactive secondary alcohols. The synthetic utility of the newly developed alpha- and beta-directing L-Rha donors 1h and 1e has been demonstrated by the efficient synthesis of a structurally unique trisaccharide 9, which is derived from the cell wall polysaccharide of Sphaerotilus natans.

Recommanded Product: Pyrazine-2-carboxylic acid. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Lei, JC; Ruan, YX; Luo, S; Yang, JS or concate me.

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

An article Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers in Vitro and in Vivo WOS:000526404600023 published article about AUREUS STRESS TOLERANCE; STAPHYLOCOCCUS-AUREUS; PROTEASE; INSIGHTS; CLEAVAGE; REVEAL; ROLES 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 in 2020, Cited 53. 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

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.. SDS of cas: 98-97-5

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

Safety of Pyrazine-2-carboxylic acid. In 2019 OPT MATER published article about BIOLOGICAL EVALUATION; ORGANIC FRAMEWORKS; COMPLEXES; ANTICANCER; POLYMERS; DERIVATIVES; COPPER; DRUGS; PHOTOLUMINESCENCE; HETEROCYCLES in [Wang, Yong-Tao; Wu, Yu-Song; Tang, Gui-Mei] Qilu Univ Technol, Shandong Acad Sci, Dept Chem Engn, Jinan 250353, Shandong, Peoples R China in 2019, Cited 103. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A set of new salts containing benzimidazole and pyrazine groups, namely, [HPZBI]X-+(-) nH(2)O (X = Cl (n = 1) (1), NO3 (n = 1) (2), ClO4 (n = 0) (3) and H2PO4 (n = 0) (4)) [PZBI = 2-(pyrazin-2-yl)-1H-benzimidazole], were obtained by the reaction of PZBI and a set of inorganic acid, respectively. The emission maxima can be found at 444, 472, 471, 432 and 443 nm for PZBI and its compounds 1-4 in the solid state at room temperature, respectively. Compared with the free PZBI, the emission maxima of compounds 1-4 are obviously blue/red-shifted for 1-4, indicating that the emission maxima are relative to the intermolecular packing distances. Their photoluminescent lifetime and quantum yield are 1.10 ns and 24.5% for 1, 0.99 ns and 26.4% for 2, 0.94 ns and 21.65% for 3, 2.86 ns and 20.57% for 4, respectively. Compounds 1-4 were structurally characterized by X-ray single crystal diffraction, FT-IR, and UV-Vis spectra. Single crystal X-ray diffraction reveals that pi center dot center dot center dot pi packing interactions and a set of hydrogen bonds can be observed. The shortest distances of pi center dot center dot center dot pi stacking interactions are 3.613, 3.534, 3.731 and 3.492 angstrom in compounds 1-4, respectively. Additionally, the thermal stabilities of compounds 1-4 were investigated in detail.

Safety of Pyrazine-2-carboxylic acid. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Wang, YT; Wu, YS; Tang, GM or concate me.

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

Recently I am researching about SUSCEPTIBILITY; IMMUNOASSAY, Saw an article supported by the Wellcome TrustWellcome TrustEuropean Commission [099805/Z/112/Z]. Published in PUBLIC LIBRARY SCIENCE in SAN FRANCISCO ,Authors: Florentini, EA; Angulo, N; Gilman, RH; Alcantara, R; Roncal, E; Antiparra, R; Toscano, E; Vallejos, K; Kirwan, D; Zimic, M; Sheen, P. 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

Pyrazinamide (PZA) susceptibility testing in Mycobacterium tuberculosis (Mtb) is a current area of development and PZA-resistant strains are increasingly prevalent. Previous studies have demonstrated that the detection of pyrazinoic acid (POA), the metabolite produced by the deamidation of PZA, is a good predictor for PZA resistance since a resistant strain would not convert PZA into POA at a critical required rate, whereas a susceptible strain will do, expelling POA to the extracellular environment at a certain rate, and allowing for quantification of this accumulated analyte. In order to quantify POA, an indirect competitive ELISA (icELISA) test using hyperimmune polyclonal rabbit serum against POA was developed: for this purpose, pure POA was first covalently linked to the highly immunogenic Keyhole Limpet Hemocyanine, and inoculated in rabbits. A construct made of bovine serum albumin (BSA) linked to pure POA and fixed at the bottom of wells was used as a competitor against spiked samples and liquid Mtb culture supernatants. When spiked samples (commercial POA alone) were analyzed, the half maximal inhibitory concentration (IC50) was 1.16 mg/mL, the limit of detection 200 mu g/mL and the assay was specific (it did not detect PZA, IC50 > 20 mg/mL). However, culture supernatants (7H9-OADC-PANTA medium) disrupted the competition and a proper icELISA curve was not obtainable. We consider that, although we have shown that it is feasible to induce antibodies against POA, matrix effects could damage its analytical usefulness; multiple, upcoming ways to solve this obstacle are suggested.

Product Details of 98-97-5. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Florentini, EA; Angulo, N; Gilman, RH; Alcantara, R; Roncal, E; Antiparra, R; Toscano, E; Vallejos, K; Kirwan, D; Zimic, M; Sheen, P or concate me.

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

In 2021 EUR J ORG CHEM published article about ONE-POT SYNTHESIS; MULTICOMPONENT REACTIONS; POSTCONDENSATION MODIFICATIONS; BUILDING-BLOCKS; SOLID-STATE; ISOCYANIDE; HEXAMETHYLENETETRAMINE; CHEMISTRY; AMMONIA; MECHANISM in [Rosalba, Thaissa Pasquali F.; Kas, Samia Sayegh A.; Sampaio, Ana Beatriz S.; Salvador, Carlos Eduardo M.; Andrade, Carlos Kleber Z.] Univ Brasilia, Inst Quim, Lab Quim Metodol & Organ Sintet LaQMOS, Campus Univ, BR-70904970 Brasilia, DF, Brazil in 2021, Cited 98. 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

Ugi reactions are still a challenge when the concomitant use of ammonia and formaldehyde is required. Herein, we propose a strategy to overcome this challenge using hexamethylenetetramine (HMTA) as a singular key for the employment of these two simple starting materials in the Ugi reaction. Acylaminoacetamide derivatives were prepared in good to excellent yields by this new methodology. The scope and optimization of the reaction conditions were investigated. This novel methodology was successfully applied in the synthesis of two different diketopiperazines (DKPs) using the Ugi/Deprotection+Activation/Cyclization (UDAC) method. A continuous flow approach was also used in this methodology.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Rosalba, TPF; Kas, SSA; Sampaio, ABS; Salvador, CEM; Andrade, CKZ or concate me.. Safety of Pyrazine-2-carboxylic acid

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

Recommanded Product: Pyrazine-2-carboxylic acid. In 2020 CRYST GROWTH DES published article about HALIDE ION SYNTHON; CRYSTAL-STRUCTURES; INTERMOLECULAR INTERACTIONS; HYDROGEN-BONDS; MOLECULES; HIERARCHY; CROSSOVER; LIGANDS; METALS; BR in [Khavasi, Hamid Reza; Gholami, Akram; Hosseini, Mahdieh; Nikpoor, Leyla] Shahid Beheshti Univ, Dept Inorgan Chem & Catalysis, Tehran 1983963113, Iran; [Eskandari, Kiamars] Isfahan Univ Technol, Dept Chem, Esfahan 8415683111, Iran in 2020, Cited 45. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A family of 10 compounds, each containing a MX2-pyrazine carboxylate complex anion and a protonated halo- (X’-) amino pyridine cation (MX2 = ZnCl2, ZnBr2, ZnI2, HgBr2, and HgI2; X’ = Cl, Br, I), are presented; a suitable system for pursuing C-X’center dot center dot center dot X-M halogen bonding (XB). The influence of halogen manipulation, metal ion and coordination variation on the nature and strength of C-X’center dot center dot center dot X-M interactions was discussed in terms of geometrical parameters, binding energies and charge density analysis with emphasis on the Laplacian of the electron density, del(2)rho. Interplay of XBs with other noncovalent interactions, mainly N-H center dot center dot center dot XM and N-py-H+center dot center dot center dot O- bonds, in supramolecular assemblies, were also investigated. The C-X’center dot center dot center dot X-M and N-H center dot center dot center dot X-M bonds have rationally been modified in strength upon changing the halogens involved, leading to systematic variations in the crystal packing.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Khavasi, HR; Gholami, A; Hosseini, M; Nikpoor, L; Eskandari, K or concate me.. Recommanded Product: Pyrazine-2-carboxylic acid

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

An 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 WOS:000555606100001 published article about PARKINSONS-DISEASE; DERIVATIVES; SAFINAMIDE; TARGETS; OPTIMIZATION; SEMBRAGILINE; PHARMACOLOGY; MODELS; POTENT in [Elkamhawy, Ahmed; Lee, Kyeong; Pae, Ae Nim; Park, Ki Duk] Dongguk Univ Seoul, Coll Pharm, Goyang 10326, South Korea; [Elkamhawy, Ahmed] Mansoura Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Mansoura, Egypt; [Paik, Sora; Roh, Eun Joo] Korea Inst Sci & Technol KIST, Chem Kin Res Ctr, Seoul 02792, South Korea; [Kim, Hyeon Jeong; Park, Jong-Hyun; Londhe, Ashwini M.] Korea Inst Sci & Technol KIST, Convergence Res Ctr Diag Treatment & Care Syst De, Seoul, South Korea; [Kim, Hyeon Jeong] Yonsei Univ, Dept Biotechnol, Seoul, South Korea; [Londhe, Ashwini M.; Pae, Ae Nim; Park, Ki Duk; Roh, Eun Joo] Korea Univ Sci & Technol, KIST Sch, Div Biomed Sci & Technol, Seoul, South Korea; [Park, Ki Duk] Kyung Hee Univ, KHU KIST Dept Converging Sci & Technol, Seoul, South Korea in 2020, Cited 52. Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

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.

Formula: C5H4N2O2. 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.

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

Recently I am researching about CROSS-COUPLING REACTIONS; CARBOXYLIC-ACIDS; QUINOLINE; SITE; DERIVATIVES; CARBONYLATION; COMPLEXES; RECEPTOR, Saw an article supported by the Education Department of Henan Province [20 A210023]; Henan Agricultural University [30500567, 30500701]; Key Science and the Technology Program of Science and Technology Department of Henan Province [152102210058, 122102210129]. Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Hu, JY; Ye, XF; Hao, S; Zhao, QR; Zhao, MQ; Wei, YW; Wu, ZY; Wang, N; Ji, XM. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid. Formula: C5H4N2O2

A highly efficient and simple procedure for the synthesis quinoline-3-carboxamides and their analogues via amidation reaction of quinoline-3-carboxylic acids with tetraalkylthiuram disulfides has been developed. The reaction proceeds efficiently under simple reaction conditions and features the generality of broad scope of substrates with good yields. This protocol provides a convenient procedure for the synthesis of various aza-heteroaromatic carboxamides, which is of pharmaceutical interest.

Formula: C5H4N2O2. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Hu, JY; Ye, XF; Hao, S; Zhao, QR; Zhao, MQ; Wei, YW; Wu, ZY; Wang, N; Ji, XM or concate me.

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

Hassan, NW; Saudi, MN; Abdel-Ghany, YS; Ismail, A; Elzahhar, PA; Sriram, D; Nassra, R; Abdel-Aziz, MM; El-Hawash, SA 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 published Novel pyrazine based anti-tubercular agents: Design, synthesis, biological evaluation and in silico studies in 2020, Cited 84. 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.

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.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Hassan, NW; Saudi, MN; Abdel-Ghany, YS; Ismail, A; Elzahhar, PA; Sriram, D; Nassra, R; Abdel-Aziz, MM; El-Hawash, SA 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. Recently I am researching about ACID-DERIVATIVES; IN-VIVO, Saw an article supported by the Sapienza Funding. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,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. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

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. About Pyrazine-2-carboxylic acid, 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 concate me.. Recommanded Product: 98-97-5

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