Month: December 2021

An article LMP2 Inhibitors as a Potential Treatment for Alzheimer’s Disease WOS:000526405300024 published article about ANTIINFLAMMATORY DRUGS; IMMUNOPROTEASOME; DESIGN; CELLS; RISK in [Bhattarai, Deepak; Lee, Min Jae; Miller, Zachary; Kim, Kyung Bo] Univ Kentucky, Dept Pharmaceut Sci, Lexington, KY 40536 USA; [Baek, Ahruem; Baek, Yu Mi; Kim, Dong-Eun] Konkuk Univ, Dept Biosci & Biotechnol, Seoul 05029, South Korea; [Yeo, In Jun; Hong, Jin Tae] Chungbuk Natl Univ, Coll Pharm, Cheongju 28160, Chungbuk, South Korea; [Lee, Sukyeong] Baylor Coll Med, Verna & Marrs McLean Dept Biochem & Mol Biol, Houston, TX 77030 USA in 2020, Cited 43. 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

The immunoproteasome (iP), an inducible proteasome variant harboring three immunosubunits, low molecular mass polypeptide-2 (LMP2), multicatalytic endopeptidase complex subunit-1, and low molecular mass polypeptide-7 (LMP7), is involved in multiple facets of inflammatory responses. We recently reported that YU102, a dual inhibitor of the iP subunit LMP2 and the constitutive proteasome catalytic subunit beta 1, ameliorates cognitive impairments in mouse models of Alzheimer’s disease (AD) independently of amyloid deposits. To investigate whether inhibition of LMP2 is sufficient to improve the cognitive functions of AD mice, here we prepared 37 YU102 analogues and identified a potent LMP2 inhibitor DB-310 (28) (IC50: 80.6 nM) with improved selectivity and permeability in cells overexpressing ABCB1 transporters. We show that DB-310 induces suppression of IL-1 alpha production in microglia cells and improves cognitive functions in the Tg2576 transgenic mouse model of AD. This study supports that inhibition of LMP2 is a promising therapeutic strategy for treatment of AD.

Application In Synthesis of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Bhattarai, D; Lee, MJ; Baek, A; Yeo, IJ; Miller, Z; Baek, YM; Lee, S; Kim, DE; Hong, JT; Kim, KB or send Email.

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

Quality Control of 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.

Quality Control 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

Computed Properties of C5H4N2O2. I found the field of Pharmacology & Pharmacy very interesting. Saw the article Identification of a Potent Oridonin Analogue for Treatment of Triple-Negative Breast Cancer published in 2020, Reprint Addresses Xu, ST; Xu, JY (corresponding author), China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Peoples R China.; Xu, ST; Xu, JY (corresponding author), China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid.

Triple-negative breast cancer (TNBC) is one of the most highly invasive and metastatic breast cancers without safe and effective therapeutic drugs. The natural product oridonin is reported to be a potential anti-TNBC agent. However, its moderate activity and complex structure hampered its clinical application. In this study, the novel oridonin analogues were first identified by removal of multiple hydroxyl groups and structural simplification of oridonin. The representative analogue 20 exhibited potent anticancer effects. Further structural modification on 20 generated the most potent derivative 56, which possessed 120-fold more potent antiproliferative activity than oridonin in the TNBC cell line HCC1806. Importantly, compound 56 exhibited more potent anticancer activity than paclitaxel in TNBC xenograft nude mice. Moreover, 56 could attenuate the expression of MMP-2, MMP-9, p-FAK, and integrin beta 1 to inhibit TNBC cell metastasis. All results suggest that compound 56 may warrant further investigation as a promising candidate agent for the treatment of TNBC.

Computed Properties of 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

In 2020 ORG LETT published article about PHASE-II TRIAL; ORGANIC SULFUR CHEMISTRY; QUINOXALINE ANTIBIOTICS; TRIOSTIN; HYPOXIA; DESULFURIZATION; DEPSIPEPTIDES; QUINOMYCIN; PATHWAY in [Ichikawa, Satoshi] Hokkaido Univ, Global Inst Collaborat Res & Educ GI CoRE, Fac Pharmaceut Sci, Ctr Res & Educ Drug Discovery, Sapporo, Hokkaido 0600812, Japan; [Ichikawa, Satoshi] Hokkaido Univ, Global Inst Collaborat Res & Educ GI CoRE, Global Stn Biostofaces & Drug Discovery, Sapporo, Hokkaido 0600812, Japan; [Kojima, Keita; Yakushiji, Fumika; Katsuyama, Akira] Hokkaido Univ, Fac Pharmaceut Sci, Sapporo, Hokkaido 0600812, Japan; [Yakushiji, Fumika; Katsuyama, Akira] Hokkaido Univ, Fac Pharmaceut Sci, Ctr Res & Educ Drug Discovery, Sapporo, Hokkaido 0600812, Japan in 2020, Cited 32. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. COA of Formula: C5H4N2O2

The first total synthesis of echinomycin (1) was accomplished by featuring the late-stage construction of the thioacetal moiety via Pummerer rearrangement and simultaneous cyclization, as well as two-directional elongation of the peptide chains to construct a C2-symmetrical bicyclic octadecadepsipeptide bridged with a sulfide linkage. This strategy can be applicable to a variety of echinomycin analogues.

COA of 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

An article Cobalt-Catalyzed Direct Carbonylative Synthesis of Free (NH)-Benzo[cd]indol-2(1H)-ones from Naphthylamides WOS:000476957200067 published article about BASIC SIDE-CHAINS; C-H CARBONYLATION; OXIDATIVE CARBONYLATION; DESIGN; C(SP(2))-H; INHIBITORS; BONDS; OPTIMIZATION; CYCLIZATION; ACTIVATION in [Ying, Jun; Fu, Lu-Yang; Zhong, Guoqiang; Wu, Xiao-Feng] Zhejiang Sci Tech Univ, Dept Chem, Xiasha Campus, Hangzhou 310018, Peoples R China; [Wu, Xiao-Feng] Univ Rostock, Leibniz Inst Katalyse eV, Albert Einstein Str 29a, D-18059 Rostock, 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. Application In Synthesis of Pyrazine-2-carboxylic acid

A cobalt-catalyzed C-H carbonylation of naphthylamides for the synthesis of benzo[cd]indol-2(1H)-one scaffolds has been developed. The reaction employs a traceless directing group and uses benzene-1,3,5-triyltriormate as the CO source, affording various free (NH)-benzo[cd]indol-2(1H)-ones in moderate to high yields (up to 88%). Using this protocol, the total synthesis of BET bromodomain inhibitors A and B was accomplished as well.

Application In Synthesis 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

Category: Pyrazines. 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.

Welcome to talk about 98-97-5, If you have any questions, you can contact Dong, XW; Zhang, JK; Xu, L; Che, JX; Cheng, G; Hu, XB; Sheng, L; Gao, AH; Li, J; Liu, T; Hu, YZ; Zhou, YB or send Email.. Category: Pyrazines

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. 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. Computed Properties of C5H4N2O2

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.

Computed Properties of 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 BIOLOGICAL EVALUATION; ORGANIC FRAMEWORKS; COMPLEXES; ANTICANCER; POLYMERS; DERIVATIVES; COPPER; DRUGS; PHOTOLUMINESCENCE; HETEROCYCLES, Saw an article supported by the Project of Shandong Province Higher Educational Science and Technology Program [J09LB03]; Shandong Distinguished Middle-aged Young Scientist Encouragement and Reward Foundation [BS2011CL034]; Shandong Provincial Natural Science FoundationNatural Science Foundation of Shandong Province [ZR2017MB041]. Published in ELSEVIER in AMSTERDAM ,Authors: Wang, YT; Wu, YS; Tang, GM. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid. HPLC of Formula: C5H4N2O2

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.

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.. HPLC of Formula: C5H4N2O2

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

Product Details of 98-97-5. In 2019 MOLECULES 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.

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.. Product Details of 98-97-5

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

Quality Control of Pyrazine-2-carboxylic acid. In 2019 J PESTIC SCI published article about ACYL-COA; ASPERGILLUS-FUMIGATUS; CHEMICAL-MODIFICATION; STRUCTURE ELUCIDATION; INHIBITORS; POTENT; RESISTANCE; METABOLITE in [Guro, Kimihiko; Horikoshi, Ryo; Nakamura, Satoshi; Mitomi, Masaaki; Oyama, Kazuhiko] Meiji Seika Pharma Co Ltd, Agr & Vet Div, Agr & Vet Res Labs, Kohoku Ku, 760 Morooka Cho, Yokohama, Kanagawa, Japan; [Hirose, Tomoyasu; Sunazuka, Toshiaki; Omura, Satoshi] Kitasato Univ, Kitasato Inst Life Sci, Grad Sch Infect Control Sci, Tokyo, Japan in 2019, Cited 22. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Pyripyropene A (PP-A), a secondary metabolite produced by filamentous fungi, shows insecticidal activity against agricultural insect pests. Synthesized PP derivatives also show a narrow insecticidal spectrum but high insecticidal activities against such sucking pests. PP-A has a low eco-toxicological impact and satisfies a prerequisite for next-generation insecticides. We investigated the effects of conversion of the 3-pyridyl and a-pyrone rings to other rings, as well as the effects of esterification, dehydration, and oxidization at the C-13 position in natural PP analogues, on the insecticidal activity and spectrum. The conversions of the 3-pyridyl and alpha-pyrone rings markedly reduced the insecticidal activity with a minimal impact on the spectrum, indicative of an important role for these rings in insecticidal activity. Some derivatives with modified structures at the C-13 position showed a higher inhibitory effect on the motility of canine heartworms and mosquito vectors than did PP-A, suggesting their utility as filaria control drugs.

Welcome to talk about 98-97-5, If you have any questions, you can contact Guro, K; Horikoshi, R; Nakamura, S; Mitomi, M; Oyama, K; Hirose, T; Sunazuka, T; Omura, S or send Email.. Quality Control of Pyrazine-2-carboxylic acid

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