Month: November 2022

In 2022,Kardashliev, Tsvetan; Panke, Sven; Held, Martin published an article in Green Chemistry. The title of the article was 《Efficient synthesis of 2,6-bis(hydroxymethyl)pyridine using whole-cell biocatalysis》.Application In Synthesis of 2,6-Pyridinedimethanol The author mentioned the following in the article:

We demonstrate a novel one-pot biocatalytic process for the preparation of a versatile chem. intermediate, 2,6-bis(hydroxymethyl)pyridine, from naturally-occurring 2,6-lutidine using recombinant microbial whole cells as a catalysts. After scale up, the bioconversion enabled titers exceeding 12 g L-1 with a space-time yield of 0.8 g L-1 h-1. This biocatalytic route offers a simpler and more sustainable alternative to multistep organic synthesis protocols.2,6-Pyridinedimethanol(cas: 1195-59-1Application In Synthesis of 2,6-Pyridinedimethanol) was used in this study.

2,6-Pyridinedimethanol(cas: 1195-59-1) belongs to pyridine. Pyridine’s structure is isoelectronic with that of benzene, but its properties are quite different. Pyridine is completely miscible with water, whereas benzene is only slightly soluble. Like all hydrocarbons, benzene is neutral (in the acid–base sense), but because of its nitrogen atom, pyridine is a weak base.Application In Synthesis of 2,6-Pyridinedimethanol

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In 2022,Djeujo, Francine Medjiofack; Francesconi, Valeria; Gonella, Maddalena; Ragazzi, Eugenio; Tonelli, Michele; Froldi, Guglielmina published an article in Molecules. The title of the article was 《Anti-α-Glucosidase and Antiglycation Activities of α-Mangostin and New Xanthenone Derivatives: Enzymatic Kinetics and Mechanistic Insights through In Vitro Studies》.Reference of 3-Aminopropan-1-ol The author mentioned the following in the article:

Diabetes mellitus is characterized by chronic hyperglycemia that promotes ROS formation, causing severe oxidative stress. Furthermore, prolonged hyperglycemia leads to glycation reactions with formation of AGEs that contribute to a chronic inflammatory state. This research aims to evaluate the inhibitory activity of α-mangostin and four synthetic xanthenone derivatives against glycation and oxidative processes and on α-glucosidase, an intestinal hydrolase that catalyzes the cleavage of oligosaccharides into glucose mols., promoting the postprandial glycemic peak. Antiglycation activity was evaluated using the BSA assay, while antioxidant capacity was detected with the ORAC assay. The inhibition of α-glucosidase activity was studied with multispectroscopic methods along with inhibitory kinetic anal. α-Mangostin and synthetic compounds at 25 μM reduced the production of AGEs, whereas the α-glucosidase activity was inhibited only by the natural compound α-Mangostin decreased enzymic activity in a concentration-dependent manner in the micromolar range by a reversible mixed-type antagonism. CD revealed a rearrangement of the secondary structure of α-glucosidase with an increase in the contents of α-helix and random coils and a decrease in β-sheet and β-turn components. The data highlighted the anti-α-glucosidase activity of α-mangostin together with its protective effects on protein glycation and oxidation damage.3-Aminopropan-1-ol(cas: 156-87-6Reference of 3-Aminopropan-1-ol) was used in this study.

3-Aminopropan-1-ol(cas: 156-87-6) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Reference of 3-Aminopropan-1-ol

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In 2022,Kim, Woojoo E.; Ishikawa, Fumihiro; Re, Rebecca N.; Suzuki, Takehiro; Dohmae, Naoshi; Kakeya, Hideaki; Tanabe, Genzoh; Burkart, Michael D. published an article in RSC Chemical Biology. The title of the article was 《Developing crosslinkers specific for epimerization domain in NRPS initiation modules to evaluate mechanism》.Category: alcohols-buliding-blocks The author mentioned the following in the article:

Nonribosomal peptide synthetases (NRPSs) are complex multi-modular enzymes containing catalytic domains responsible for the loading and incorporation of amino acids into natural products. These unique mol. factories can produce peptides with nonproteinogenic D-amino acids in which the epimerization (E) domain catalyzes the conversion of L-amino acids to D-amino acids, but its mechanism remains not fully understood. Here, we describe the development of pantetheine crosslinking probes that mimic the natural substrate L-Phe of the initiation module of tyrocidine synthetase, TycA, to elucidate and study the catalytic residues of the E domain. Mechanism-based crosslinking assays and MALDI-TOF MS were used to identify both H743 and E882 as the crosslinking site residues, demonstrating their roles as catalytic bases. Mutagenesis studies further validated these results and allowed the comparison of reactivity between the catalytic residues, concluding that glutamate acts as the dominant nucleophile in the crosslinking reaction, resembling the deprotonation of the Cα-H of amino acids in the epimerization reaction. The crosslinking probes employed in these studies provide new tools for studying the mol. details of E domains, as well as the potential to study C domains. In particular, they would elucidate key information for how these domains function and interact with their substrates in nature, further enhancing the knowledge needed to assist combinatorial biosynthetic efforts of NRPS systems to produce novel compounds In the experiment, the researchers used 4-Aminobutan-1-ol(cas: 13325-10-5Category: alcohols-buliding-blocks)

4-Aminobutan-1-ol(cas: 13325-10-5) is used in the synthesis of NSAIDs with anti-inflammatory properties. Also used in the synthesis of polyamine transport ligands with specificity against human cancers allowing easy access to specific cancer cells.Category: alcohols-buliding-blocks

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In 2022,Scarneo, Scott; Hughes, Philip; Freeze, Robert; Yang, Kelly; Totzke, Juliane; Haystead, Timothy published an article in ACS Chemical Biology. The title of the article was 《Development and Efficacy of an Orally Bioavailable Selective TAK1 Inhibitor for the Treatment of Inflammatory Arthritis》.Application of 27489-62-9 The author mentioned the following in the article:

Selective targeting of TNF in inflammatory diseases such as rheumatoid arthritis (RA) has provided great therapeutic benefit to many patients with chronic RA. Although these therapies show initially high response rates, their therapeutic benefit is limited over the lifetime of the patient due to the development of antidrug antibodies that preclude proper therapeutic benefits. As a result, patients often return to more problematic therapies such as methotrexate or hydroxychloroquine, which carry long-term side effects. Thus, there is an unmet medical need to develop alternative treatments enabling patients to regain the benefits of selectively targeting TNF functions in vivo. The protein kinase TAK1 is a critical signaling node in TNF-mediated intracellular signaling, regulating downstream NF-κβ activation, leading to the transcription of inflammatory cytokines. TAK1 inhibitors have been developed but have been limited in their clin. advancement due to the lack of selectivity within the human kinome and, most importantly, lack of oral bioavailability. Using a directed medicinal chem. approach, driven by the cocrystal structure of the TAK1 inhibitor takinib, we developed HS-276 (I), a potent (Ki = 2.5 nM) and highly selective orally bioavailable TAK1 inhibitor. Following oral administration in normal mice, HS-276 is well tolerated (MTD >100 mg/Kg), displaying >95% bioavailability with μM plasma levels. The in vitro and in vivo efficacy of HS-276 showed significant inhibition of TNF-mediated cytokine profiles, correlating with significant attenuation of arthritic-like symptoms in the CIA mouse model of inflammatory RA. Our studies reinforce the hypothesis that TAK1 can be safely targeted pharmacol. to provide an effective alternative to frontline biol.-based RA therapeutics.trans-4-Aminocyclohexanol(cas: 27489-62-9Application of 27489-62-9) was used in this study.

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Application of 27489-62-9

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Reference of 2,6-PyridinedimethanolIn 2019 ,《Site-Specific Modification of Proteins through N-Terminal Azide Labeling and a Chelation-Assisted CuAAC Reaction》 appeared in Bioconjugate Chemistry. The author of the article were Inoue, Nozomu; Onoda, Akira; Hayashi, Takashi. The article conveys some information:

Site-specific modification of peptides and proteins is an important method for introducing an artificial function to the protein surface. Recently, we found that new bioconjugation reagents, 6-(azidomethyl)-2-pyridinecarbaldehyde (6AMPC) derivatives, allow specific N-terminal modification and enhance the reaction rate of the subsequent bioconjugation in a chelation-assisted CuAAC reaction. The N-terminal specific azide-labeling of bioactive peptides and proteins occurs under mild reaction conditions with 6AMPC derivatives (angiotensin I: 90%, RNase A: 90%). Kinetic anal. of the CuAAC reaction with azide-labeled proteins reveals that the ligation is promoted in the presence of a copper-chelating pyridine moiety. Importantly, the introduction of an electron-donating methoxy group to the pyridine moiety further accelerates the CuAAC ligation. We demonstrate that this method enables site-specific conjugation of various functional mols. such as fluorophores, biotin, and polyethylene glycol. In the experiment, the researchers used many compounds, for example, 2,6-Pyridinedimethanol(cas: 1195-59-1Reference of 2,6-Pyridinedimethanol)

2,6-Pyridinedimethanol(cas: 1195-59-1) belongs to pyridine. The basicity and metallophilic high donor number of these π-deficient systems has long favored them as ligands in metal catalysis. The last decade saw pyridine assume a stronger role as functional group for directed C–H oxidation/activation.Reference of 2,6-Pyridinedimethanol

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Recommanded Product: 4048-33-3In 2019 ,《Synthesis of neuraminidase-resistant sialoside-modified three-way junction DNA and its binding ability to various influenza viruses》 was published in Carbohydrate Research. The article was written by Yamabe, Miyuki; Fujita, Akira; Kaihatsu, Kunihiro; Ebara, Yasuhito. The article contains the following contents:

Natural sialic acid-modified compounds are capable of targeting influenza virus hemagglutinin (HA). However, these compounds have limited inhibitory effect because natural O-glycoside bond in these compounds are prone to be cleaved by neuraminidase (NA) on the surface of viruses. In this study, we synthesized NA-resistant sialoside that included unnatural S-glycoside bonds and modified this sialoside on a three-way junction (3WJ) DNA to display complementary distribution to its binding sites on a HA trimer. This S-glycoside-containing sialoside-modified 3WJ DNA showed certain NA resistance and maintained high binding affinity. Importantly, our observations showed that substituting natural O-glycoside with unnatural S-glycoside did not affect the binding affinity of the sialoside-modified 3WJ DNA for viruses. Thus, this study is an important step forward in the development of NA-resistant sialoside derivatives for more effective detection and inhibition of infection by a broad spectrum of viruses. In the part of experimental materials, we found many familiar compounds, such as 6-Aminohexan-1-ol(cas: 4048-33-3Recommanded Product: 4048-33-3)

6-Aminohexan-1-ol(cas: 4048-33-3) can undergo cyclization over copper supported on γ-alumina and magnesia to form hexahydro-1H-azepine. It may be used along with glutaric acid to generate poly(ester amide)s with excellent film- and fiber forming properties.Recommanded Product: 4048-33-3

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Electric Literature of C7H6O3In 2020 ,《Synthesis of symmetrical bis-Schiff base-disulfide hybrids as highly effective anti-leishmanial agents》 was published in Bioorganic Chemistry. The article was written by Taha, Muhammad; Sain, Amyra Amat; Ali, Muhammad; Anouar, El Hassane; Rahim, Fazal; Ismail, Nor Hadiani; Adenan, Mohd Ilham; Imran, Syahrul; Al-Harrasi, Ahmed; Nawaz, Fasial; Iqbal, Naveed; Khan, Khalid Mohammed. The article contains the following contents:

Leishmaniasis has affected a wider part of population around the globe. Most often, the existing regiments to battle against leishmaniasis are inadequate and limited. In our ongoing efforts to develop new leishmanicidal agents, we have synthesized a series of novel and sym. bis-Schiff base-disulfide hybrids 1-27. Intermediate disulfide was synthesized from corresponding 2-aminothiol followed by reacting the coupled adduct with various aromatic aldehydes. All these compounds showed outstanding inhibition when compared with standard (Table 1). Out of twenty seven analogs, twenty two analogs i.e. 1-5, 7-13, 17-21, 23-27 analogs showed excellent inhibitory potential with EC50 values ranging from 0.010 ± 0.00 to 0.096 ± 0.01μM while five compounds i.e. 6, 14-16, and 22 showed good inhibitory potential with EC50 values ranging from 0.10 ± 0.00 to 0.137 ± 0.01μM when compared with the standard Amphotericin B. Structure-activity relationship has been established while mol. docking studies were performed to pin the binding interaction of active mols. This study will help to develop new antileishmanial lead compounds In addition to this study using 3,5-Dihydroxybenzaldehyde, there are many other studies that have used 3,5-Dihydroxybenzaldehyde(cas: 26153-38-8Electric Literature of C7H6O3) was used in this study.

3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is a building block. It has been used in the synthesis of 2,4-dimethylbenzoylhydrazones with antileishmanial and antioxidant activities.Electric Literature of C7H6O3

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Application of 873-75-6In 2019 ,《Iridium-Catalyzed Alkylation of Amine and Nitrobenzene with Alcohol to Tertiary Amine under Base- and Solvent-Free Conditions》 was published in Journal of Organic Chemistry. The article was written by Li, Chao; Wan, Ke-feng; Guo, Fu-ya; Wu, Qian-hui; Yuan, Mao-lin; Li, Rui-xiang; Fu, Hai-yan; Zheng, Xue-li; Chen, Hua. The article contains the following contents:

Herein, an efficient and green method for the selective synthesis of tertiary amines has been developed that involves iridium-catalyzed alkylation of various primary amines with aromatic or aliphatic alcs. Notably, the catalytic protocol enables this transformation in the absence of addnl. base and solvent. Furthermore, the alkylation of nitrobenzene with primary alc. to tertiary amine has also been achieved by the same catalytic system. Deuterium-labeling experiments and a series of control experiments were conducted, and the results suggested that an intermol. borrowing hydrogen pathway might exist in the alkylation process. The results came from multiple reactions, including the reaction of (4-Bromophenyl)methanol(cas: 873-75-6Application of 873-75-6)

(4-Bromophenyl)methanol(cas: 873-75-6) undergoes three-component reaction with acetylferrocene and arylboronic acid to give ferrocenyl ketones containing biaryls.Application of 873-75-6 It undergoes oxidation reaction in the presence of polyvinylpolypyrrolidone-supported hydrogen peroxide, silica sulfuric acid and ammonium bromide to yield 4-bromobenzaldehyde.

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《3-Amino-1-propanol and N-methylaminoethanol: coordination to zinc(II) vs. decomposition to ammonia》 was written by Podjed, Nina; Stare, Petra; Korosec, Romana Cerc; Alcaide, Maria M.; Lopez-Serrano, Joaquin; Modec, Barbara. Related Products of 156-87-6This research focused onzinc quinaldinate aminopropanol methylaminoethanol ammonia complex preparation crystal structure; DFT calculation zinc quinaldinate aminopropanol methylaminoethanol ammonia complex. The article conveys some information:

To broaden the limited knowledge concerning the zinc(II) coordination chem. with amino alcs., reactions of [Zn(quin)2(H2O)] (quin- = quinaldinate, C10H6NO2) with 3-amino-1-propanol (3-apOH, C3H9NO) and N-methylaminoethanol (N-maeOH, C3H9NO) were studied. The starting material, zinc(II) with two quinaldinates coordinated in a bidentate chelating mode, provides a structurally rigid core with two sites available for interaction with amino alc. ligands. When the reactions were carried out in acetonitrile in autoclaves at 105°, an unforeseen decomposition of amino alcs. to ammonia took place. This was accompanied by crystallization of an ammine complex [Zn(quin)2(NH3)] (1). Mass spectrometry of the gaseous phases confirmed unambiguously the presence of ammonia in such reaction mixtures The desired complexes with coordinated amino alcs. could be obtained in good yield by carrying out the reactions at room temperature and/or in various solvents. Two novel amino alc. complexes were prepared, [Zn(quin)2(3-apOH)] and [Zn(quin)2(N-maeOH)]. The 3-apOH ligand was coordinated to zinc(II) in a monodentate manner via the amino nitrogen. The 3-apOH complex crystallizes as an acetonitrile (2a), ethanol (2b), 2-propanol (2c) or water (2d) solvate. The conversion of 2a to 2d was monitored by IR spectroscopy. In [Zn(quin)2(N-maeOH)] (3), the N-maeOH ligand was coordinated in a bidentate chelating manner through both functional groups. DFT calculations were performed on the isomers of [Zn(quin)2(3-apOH)] and [Zn(quin)2(N-maeOH)], which differ in the binding modes of their amino alc. ligands. Complete characterization of all compounds by x-ray structure anal., IR spectroscopy and NMR spectroscopy is presented. In the experiment, the researchers used many compounds, for example, 3-Aminopropan-1-ol(cas: 156-87-6Related Products of 156-87-6)

3-Aminopropan-1-ol(cas: 156-87-6) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Related Products of 156-87-6

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Alcohol – Wikipedia,
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《Ni-catalyzed Reductive Deaminative Arylation at sp3 Carbon Centers》 was written by Martin-Montero, Raul; Yatham, Veera Reddy; Yin, Hongfei; Davies, Jacob; Martin, Ruben. Formula: C8H19NO2 And the article was included in Organic Letters on April 19 ,2019. The article conveys some information:

A Ni-catalyzed reductive deaminative arylation at unactivated sp3 carbon centers is described. This operationally simple and user-friendly protocol exhibits excellent chemoselectivity profile and broad substrate scope, thus complementing existing metal-catalyzed cross-coupling reactions to forge sp3 C-C linkages. These virtues have been assessed in the context of late-stage functionalization, hence providing a strategic advantage to reliably generate structure diversity with amine-containing drugs. The results came from multiple reactions, including the reaction of 4,4-Diethoxybutan-1-amine(cas: 6346-09-4Formula: C8H19NO2)

4,4-Diethoxybutan-1-amine(cas: 6346-09-4) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Formula: C8H19NO2

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