Category: 98-97-5

An article Rhodium-Catalyzed Regiodivergent and Enantioselective Hydroboration of Enamides WOS:000503917800046 published article about TERTIARY BORONIC ESTERS; AMINOBORONIC ACID-DERIVATIVES; ASYMMETRIC HYDROBORATION; PINACOLBORYL ADDITION; AMINOBORATION; ALKENES; SECONDARY; HYDROFUNCTIONALIZATION; HYDROALKYNYLATION; BORYLATION in [Bai, Xiao-Yan; Zhao, Wei; Sun, Xin; Li, Bi-Jie] Tsinghua Univ, Dept Chem, CBMS, Beijing 100084, Peoples R China in 2019, Cited 89. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Formula: C5H4N2O2

Chiral alpha- and beta-aminoboronic acids exhibit unique biological activities. General methods for the synthesis of these bioisosteres of amino acids are highly desirable. We report a facile preparation of these compounds through rhodium-catalyzed regiodivergent and enantioselective hydroboration of enamides. Catalytic asymmetric synthesis of alpha- and beta-aminoboronic esters with high regio-, diastereo-, and enantioselectivities were achieved through effective catalyst control and tuning substrate geometry. Starting from easily available materials, this strategy provides a unified synthetic access to both enantioenriched alpha-boration and beta-boration products. The synthetic utility of these methods was demonstrated by efficient synthesis of an anticancer drug molecule and diverse transformations of the boration products.

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

In 2021 BIOORG CHEM published article about LEISHMANIA; INFECTION; DOCKING in [Khatoon, Saira; Hameed, Shahid; Naseer, Muhammad Moazzam] Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan; [Aroosh, Aiman; Islam, Arshad; Kalsoom, Saima; Yasinzai, Masoom] Int Islamic Univ, Fac Basic & Appl Sci, Suleiman Bin Abdullah Aba Akhail Ctr Interdiscipl, Islamabad 44000, Pakistan; [Islam, Arshad] Govt Lady Reading Hosp Med Teaching Inst, Dept Pathol, Peshawar, KPK, Pakistan; [Ahmad, Faisal] Quaid I Azam Univ, Natl Ctr Bioinformat, Islamabad 45320, Pakistan; [Abbasi, Sumra Wajid] Natl Univ Med Sci, Dept Biol Sci, Rawalpindi, Pakistan in 2021, Cited 48. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Computed Properties of C5H4N2O2

Leishmaniasis being one of the six major tropical diseases that affects nearly 0.7-1.3 million people annually, has so far limited and high toxic therapeutic options. Herein, we report the synthesis, in silico, and in vitro evaluations of novel coumarin-incorporated isatin hydrazones (Spf-1 – Spf-10) as highly potent and safe antileishmanial agents. Molecular docking was initially carried out to decipher the binding confirmation of lead molecules towards the active cavity of the target protein (Leishmanolysin gp63) of Leishmania tropica. Among all the docked compounds, only Spf-6, Spf-8, and Spf-10 showed high binding affinities due to a pattern of strong conventional hydrogen bonds and hydrophobic pi-interactions. The molecular dynamics simulations showed the stable pattern of such bonding and structure-based confirmation with a time scale of 50 ns towards the top compound (Spf-10) and protein. These analyses affirmed the high stability of the system. Three out of ten compounds evaluated for their antileishmanial activity against Leishmania tropica promastigotes and amastigotes were found to be active at micromolar concentrations (IC50 range 0.1-4.13 mu mol/L), and most importantly, they were also found to be highly biocompatible when screened for their toxicity in human erythrocytes.

Computed Properties of C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Khatoon, S; Aroosh, A; Islam, A; Kalsoom, S; Ahmad, F; Hameed, S; Abbasi, SW; Yasinzai, M; Naseer, MM or send Email.

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

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. Recommanded Product: 98-97-5, 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.

Recommanded Product: 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Yao, H; Xie, SW; Ma, XQ; Liu, JK; Wu, HY; Lin, AJ; Yao, HQ; Li, DH; Xu, ST; Yang, DH; Chen, ZS; Xu, JY or send Email.

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

In 2021 ASIAN J ORG CHEM published article about UNACTIVATED C(SP(3))-H BONDS; ENANTIOSELECTIVE SYNTHESIS; GAMMA-C(SP(3))-H BONDS; CATALYZED ARYLATION; DERIVATIVES; BIDENTATE; ALKYNYLATION; C(SP(2))-H; AFFINITY; ALCOHOLS in [Singh, Prabhakar; Arulananda Babu, Srinivasarao; Aggarwal, Yashika; Patel, Pooja] Indian Inst Sci Educ & Res IISER Mohali, Dept Chem Sci, Sect 81, Manauli Po 140306, Punjab, India in 2021, Cited 68. 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

We report the Pd(II)-catalyzed picolinamide-aided ortho-C-H arylation-, alkylation-, and halogenation (sp(2) gamma-C-H functionalization) of phenylglycinol substrates. Phenylglycinols are remarkable building blocks and have found different applications in synthetic organic and medicinal chemistry. This work is a contribution towards the expansion of the library of phenylglycinol scaffolds and also substrate scope development by using the Pd(II)-catalyzed bidentate directing group picolinamide-aided C-H activation tactic.

Recommanded Product: 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Singh, P; Babu, SA; Aggarwal, Y; Patel, P or send Email.

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

Quality Control of Pyrazine-2-carboxylic acid. Authors Swiderski, G; Kalinowska, M; Jablonska-Trypuc, A; Wolejko, E; Wydro, U; Lyszczek, R; Rusinek, I; Lewandowski, W in ELSEVIER published article about in [Swiderski, Grzegorz; Kalinowska, Monika; Jablonska-Trypuc, Agata; Wolejko, Elzbieta; Wydro, Urszula; Lewandowski, Wlodzimierz] Bialystok Tech Univ, Dept Chem Biol & Biotechnol, Wiejska 45E St, PL-15351 Bialystok, Poland; [Lyszczek, Renata; Rusinek, Iwona] UMCS, Dept Gen & Coordinat Chem, MC Sklodowska Sq 2, PL-20031 Lublin, Poland in 2021, Cited 50. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Diazinecarboxylic acids (pyridazine-3-carboxylic, pyridazine-4-carboxylic, pyrimidine-2-carboxylic, pyrimidine-4-carboxylic, pyrimidine-5-carboxylic and pyrazine-2-carboxylic acids) were characterized by means of spectroscopic (FT-Raman, FTIR, UV, (HNMR)-H-1, (CNMR)-C-13) and thermogravimetric analysis as well as antimicrobial and cytotoxic tests. The structures of diazinecarboxylic acids were calculated by the DFT method (B3LYP/6-311G(d, p). For the most stable conformers, the energy of HOMO and LUMO molecular orbitals, the geometric (HOMA, GEO, EN, I6) and magnetic (NICS) aromaticity indices, NBO electronic charge distribution, sEDA and pEDA indexes, Wiberg Bond Order, Wiberg Index and theoretical IR and NMR spectra have been calculated. The energies of protonating and deprotonating acids were also calculated. The effect of the nitrogen heteroatom position in the aromatic ring in relation to the position of the carboxyl group on the electronic charge distribution, thermal stability, antimicrobial and cytotoxicity activities of the examined acids was determined. Antimicrobial activity of tested acids against of Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosaand Candida albicanswas calculated based on MTT colorimetric assay (MCA). The cytotocic effect of diazynecarboxylic acids was examined in A375 melanoma cell line and DLD-1 cell line. A biplot analysis was performed in order to determine the correlations between selected parameters of the tested compounds and relative cell viability of E. coli, B. subtilis, P. aeruginosa, C. albicans, A375 and DLD-1 cell lines. Thermal behaviour of all investigated carboxylic acids was investigated using thermogravimetry (TG) and differential scanning calorimetry (DSC) techniques in flowing air atmosphere. All compounds are stable in room temperature. (C) 2021 Elsevier B.V. All rights reserved.

Quality Control of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Swiderski, G; Kalinowska, M; Jablonska-Trypuc, A; Wolejko, E; Wydro, U; Lyszczek, R; Rusinek, I; Lewandowski, W or send Email.

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

An article Sensing and photocatalytic properties of nanosized Cu(I)CN organotin supramolecular coordination polymer based on pyrazine WOS:000478695400001 published article about METAL-ORGANIC FRAMEWORKS; X-RAY-STRUCTURE; CRYSTAL-STRUCTURES; COPPER(I) CYANIDE; ETHYL ISONICOTINATE; SELECTIVE DETECTION; LUMINESCENT SENSOR; ANTITUMOR-ACTIVITY; BUILDING-BLOCKS; SINGLE-CRYSTAL in [Etaiw, Safaa El-din H.; Marie, Hassan; Elsharqawy, Fatma A.] Tanta Univ, Fac Sci, Chem Dept, Tanta, Egypt; [Shalaby, Elsayed M.] Natl Res Ctr, Phys Div, Xray Crystallog Lab, Cairo, Egypt; [Farag, Rabie S.] Al Azhar Univ, Fac Sci, Chem Dept, Cairo, Egypt in 2019, Cited 76. Safety of Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Orange prismatic crystals of the supramolecular coordination polymer (SCP) (3)(infinity)[Cu(CN)(2)(Me3Sn)(Pyz)], SCP1, were synthesized using a self-assembly method under ambient conditions. Nanosized 1 was obtained using the same molar ratio in water by ultrasonic irradiation. SCP1 was characterized using single-crystal X-ray diffraction, elemental analysis, thermal analysis and Fourier transform infrared spectroscopy. SCP1 and its nanosized 1 particles were also examined using powder X-ay diffraction and scanning electron microscopy. The luminescence emission of SCP1 was studied as well as its use as a sensor for the detection of common organic solvents and metal ions. Also, the catalytic activities of nanosized 1 towards various organic dyes were investigated under ambient conditions, UV irradiation and ultrasonic irradiation. Nanosized 1 as a heterogeneous nanoparticle catalyst exhibits high catalytic activity for the degradation of eosin-Y and acid blue dyes. The mechanism of degradation investigated using various scavenger techniques is proposed and discussed. The catalytic oxidation process is mainly caused by center dot OH radicals.

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

Carvalho, EM; Paulo, TD; Saquet, AS; Abbadi, BL; Macchi, FS; Bizarro, CV; Campos, RD; Ferreira, TLA; do Nascimento, NRF; Lopes, LGF; Chauvin, R; Sousa, EHS; Bernardes-Genisson, V in [Carvalho, Edinilton Muniz; Paulo, Tercio de Freitas; Saquet, Alix Sournia; Chauvin, Remi; Bernardes-Genisson, Vania] CNRS, Lab Chim Coordinat, LCC, UPR 8241, 205 Route Narbonne,BP 44099, F-31077 Toulouse 4, France; [Carvalho, Edinilton Muniz; Paulo, Tercio de Freitas; Chauvin, Remi; Bernardes-Genisson, Vania] Univ Toulouse, Univ Paul Sabatier, UPS, 118 Route Narbonne, F-31062 Toulouse 9, France; [Carvalho, Edinilton Muniz; Paulo, Tercio de Freitas; Franca Lopes, Luiz Gonzaga; Silva Sousa, Eduardo Henrique] Univ Fed Ceara, Dept Quim Organ & Inorgan, Grp Bioinorgen, Campus Pici, BR-60455760 Fortaleza, Ceara, Brazil; [Abbadi, Bruno Lopes; Macchi, Fernanda Souza; Bizarro, Cristiano Valim] Pontificia Univ Catolica Rio Grande Do Sul PUCRS, Ctr Pesquisas Biol Mol & Func CPBMF, Porto Alegre, RS, Brazil; [Abbadi, Bruno Lopes; Macchi, Fernanda Souza; Bizarro, Cristiano Valim; Franca Lopes, Luiz Gonzaga; Silva Sousa, Eduardo Henrique] Inst Nacl Ciencia & Tecnol TB INCT TB, Porto Alegre, RS, Brazil; [Campos, Rafael de Morais; Abrantes Ferreira, Talles Luann; Falcao do Nascimento, Nilberto Robson] Univ Estadual Ceara, Lab Farmacol Cardiovasc & Renal, Campus Itaperi, BR-60714903 Fortaleza, Ceara, Brazil published Pentacyanoferrate(II) complex of pyridine-4-and pyrazine-2-hydroxamic acid as source of HNO: investigation of anti-tubercular and vasodilation activities in 2020, Cited 40. Category: Pyrazines. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A pharmacophore design approach, based on the coordination chemistry of an intimate molecular hybrid of active metabolites of pro-drugs, known to release active species upon enzymatic oxidative activation, is devised. This is exemplified by combining two anti-mycobacterial drugs: pyrazinamide (first line) and delamanid (third line) whose active metabolites are pyrazinoic acid (PyzCOOH) and likely nitroxyl (HNO (or NO.)), respectively. Aiming to generate those active species, a hybrid compound was envisaged by coordination of pyrazine-2-hydroxamic acid (PyzCONHOH) with a Na-3[Fe-II(CN)(5)] moiety. The corresponding pentacyanoferrate(II) complex Na-4[Fe-II(CN)(5)(PyzCONHO(-))] was synthesized and characterized by several spectroscopic techniques, cyclic voltammetry, and DFT calculations. Chemical oxidation of this complex with H(2)O(2)was shown to induce the release of the metabolite PyzCOOH, without the need of theMycobacterium tuberculosis(Mtb) pyrazinamidase enzyme (PncA). Control experiments show that both H2O2- and N-coordinated pyrazine Fe(II)species are required, ruling out a direct hydrolysis of the hydroxamic acid or an alternative oxidative route through chelation of a metal center by a hydroxamic group. The release of HNO was observed using EPR spectroscopy in the presence of a spin trapping agent. The devised iron metal complex of pyrazine-2-hydroxamic acid was found inactive against an actively growing/non-resistantMtbstrain; however, it showed a strong dose-dependent and reversible vasodilatory activity with mostly lesser toxic effects than the reference drug sodium nitroprussiate, unveiling thus a potential indication for acute or chronic cardiovascular pathology. This is a priori a further indirect evidence of HNO release from this metal complex, standing as a possible pharmacophore model for an alternative vasodilator drug.

Category: Pyrazines. Welcome to talk about 98-97-5, If you have any questions, you can contact Carvalho, EM; Paulo, TD; Saquet, AS; Abbadi, BL; Macchi, FS; Bizarro, CV; Campos, RD; Ferreira, TLA; do Nascimento, NRF; Lopes, LGF; Chauvin, R; Sousa, EHS; Bernardes-Genisson, V or send Email.

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

Safety of Pyrazine-2-carboxylic acid. In 2019 EUR J MED CHEM published article about MECHANISMS; IDENTIFICATION; INFLAMMASOME; CHEMOTAXIS in [Zhang, Zhenguo; Lu, Ran; Jiang, Cheng] China Pharmaceut Univ, Jiang Su Key Lab Drug Design & Optimizat, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China; [Zhang, Zhenguo; Lu, Ran; Li, Baiyang; Meng, Zibo; Jiang, Cheng] China Pharmaceut Univ, Dept Med Chem, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China; [Hao, Kun] China Pharmaceut Univ, State Key Lab Nat Med, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China; [Li, Hanwen; Liu, Chunxiao; Zhou, Mengze; Hu, Qinghua] China Pharmaceut Univ, Key Lab Drug Metab & Pharmacokinet, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China in 2019, Cited 35. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

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.

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 Spectroscopic and Theoretical Investigation of Color Tuning in Deep-Red Luminescent Iridium(III) Complexes WOS:000514488400018 published article about HIGHLY EFFICIENT; METAL-COMPLEXES; QUINOXALINE LIGANDS; 1ST EXAMPLES; PHOSPHORESCENT; EMISSION; BEARING; PHOTOPHYSICS; CONVERSION; DEVICES in [Stonelake, Thomas M.; Phillips, Kaitlin A.; Otaif, Haleema Y.; Edwardson, Zachary C.; Beames, Joseph M.; Pope, Simon J. A.] Cardiff Univ, Sch Chem, Cardiff CF10 3AT, Wales; [Horton, Peter N.; Coles, Simon J.] Univ Southampton, Fac Nat & Environm Sci, UK Natl Crystallog Serv, Chem, Southampton SO17 1BJ, Hants, England in 2020, Cited 60. 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 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).

Recommanded Product: 98-97-5. 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

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers in Vitro and in Vivo published in 2020. SDS of cas: 98-97-5, Reprint Addresses Bao, R; Luo, YF (corresponding author), Sichuan Univ, State Key Lab Biotherapy, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China.; Bao, R; Luo, YF (corresponding author), Sichuan Univ, Canc Ctr, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

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.

SDS of cas: 98-97-5. 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